Month: November 2022

Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C was written by Poreba, Marcin;Mihelic, Marko;Krai, Priscilla;Rajkovic, Jelena;Krezel, Artur;Pawelczak, Malgorzata;Klemba, Michael;Turk, Dusan;Turk, Boris;Latajka, Rafal;Drag, Marcin. And the article was included in Amino Acids in 2014.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Mammalian cathepsin C is primarily responsible for the removal of N-terminal dipeptides and activation of several serine proteases in inflammatory or immune cells, while its malarial parasite ortholog dipeptidyl aminopeptidase 1 plays a crucial role in catabolizing the Hb of its host erythrocyte. In this report, we describe the systematic substrate specificity anal. of three cathepsin C orthologs from Homo sapiens (human), Bos taurus (bovine) and Plasmodium falciparum (malaria parasite). Here, we present a new approach with a tailored fluorogenic substrate library designed and synthesized to probe the S1 and S2 pocket preferences of these enzymes with both natural and a broad range of unnatural amino acids. Our approach identified very efficiently hydrolyzed substrates containing unnatural amino acids, which resulted in the design of significantly better substrates than those previously known. Addnl., in this study significant differences in terms of the structures of optimal substrates for human and malarial orthologs are important from the therapeutic point of view. These data can be also used for the design of specific inhibitors or activity-based probes. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C was written by Poreba, Marcin;Mihelic, Marko;Krai, Priscilla;Rajkovic, Jelena;Krezel, Artur;Pawelczak, Malgorzata;Klemba, Michael;Turk, Dusan;Turk, Boris;Latajka, Rafal;Drag, Marcin. And the article was included in Amino Acids in 2014.Quality Control of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Mammalian cathepsin C is primarily responsible for the removal of N-terminal dipeptides and activation of several serine proteases in inflammatory or immune cells, while its malarial parasite ortholog dipeptidyl aminopeptidase 1 plays a crucial role in catabolizing the Hb of its host erythrocyte. In this report, we describe the systematic substrate specificity anal. of three cathepsin C orthologs from Homo sapiens (human), Bos taurus (bovine) and Plasmodium falciparum (malaria parasite). Here, we present a new approach with a tailored fluorogenic substrate library designed and synthesized to probe the S1 and S2 pocket preferences of these enzymes with both natural and a broad range of unnatural amino acids. Our approach identified very efficiently hydrolyzed substrates containing unnatural amino acids, which resulted in the design of significantly better substrates than those previously known. Addnl., in this study significant differences in terms of the structures of optimal substrates for human and malarial orthologs are important from the therapeutic point of view. These data can be also used for the design of specific inhibitors or activity-based probes. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Quality Control of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Quality Control of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In silico plasma protein binding studies of selected group of drugs using TLC and HPLC retention data was written by Wanat, Karolina;Zydek, Grazyna;Hekner, Adam;Brzezinska, Elzbieta. And the article was included in Pharmaceuticals in 2021.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

Plasma protein binding is an important determinant of the pharmacokinetic properties of chem. compounds in living organisms. The aim of the present study was to determine the index of protein binding affinity based on chromatog. experiments The question is which chromatog. environment will best mimic the drug-protein binding conditions. Retention data from normal phase thin-layer liquid chromatog. (NP TLC), reversed phase (RP) TLC and HPLC chromatog. experiments with 129 active pharmaceutical ingredients (APIs) were collected. The stationary phase of the TLC plates was modified with protein and the HPLC column was filled with immobilized human serum albumin. In both chromatog. methods, the mobile phase was based on a buffer with a pH of 7.4 to mimic physiol. conditions. Chemometric analyses were performed to compare multiple linear regression models (MLRs) with retention data, using protein binding values as the dependent variable. In the course of the anal., APIs were divided into acidic, basic and neutral groups, and sep. models were created for each group. The MLR models had a coefficient of determination between 0.73 and 0.91, with the highest values from NP TLC data. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Protective effects of the soluble epoxide hydrolase inhibitor 1- trifluoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea in a rat model of permanent middle cerebral artery occlusion was written by Zhang, Linlei;Xu, Shasha;Wu, Xiaoxiao;Muse, Farah Mohamed;Chen, Jiaou;Cao, Yungang;Yan, Jueyue;Cheng, Zicheng;Yi, Xingyang;Han, Zhao. And the article was included in Frontiers in Pharmacology in 2020.Related Products of 1222780-33-7 The following contents are mentioned in the article:

Acute ischemic stroke is a serious disease that endangers human health. In our efforts to develop an effective therapy, we previously showed that the potent, highly selective inhibitor of soluble epoxide hydrolase called 1-trifuoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea (TPPU) protects the brain against focal ischemia in rats. Here we explored the mechanism of TPPU action by assessing whether it could preserve blood-brain barrier integrity and reduce apoptosis in the brain during permanent middle cerebral artery occlusion in male Sprague-Dawley rats. TPPU administration at the onset of stroke and once daily thereafter led to smaller infarct volume and brain edema as well as milder neurol. deficits. TPPU significantly inhibited the activity of soluble epoxide hydrolase and matrix metalloproteases 2 and 9, reducing 14,15-DHET levels, while increasing expression of tight junction proteins. TPPU decreased numbers of apoptotic cells by down-regulating the pro-apoptotic proteins BAX and Caspase-3, while upregulating the anti-apoptotic protein BCL-2. Our results suggest that TPPU can protect the blood-brain barrier and reduce the apoptosis of brain tissue caused by ischemia. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Related Products of 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Related Products of 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Application of 86069-86-5 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Biochar – An efficient sorption material for the removal of pharmaceutically active compounds, DNA and RNA fragments from wastewater was written by Bimova, Paula;Roupcova, Petra;Klouda, Karel;Matejova, Lenka;Stanova, Andrea Vojs;Grabicova, Katerina;Grabic, Roman;Majova, Veronika;Hives, Jan;Spalkova, Viera;Gemeiner, Pavol;Celec, Peter;Konecna, Barbora;Birosova, Lucia;Krahulcova, Monika;Mackulak, Tomas. And the article was included in Journal of Environmental Chemical Engineering in 2021.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

Wastewaters are considered a remarkable source of micropollutants capable of influencing the environment both directly and indirectly. Here we tested porous ecol. carbon (Biochar), an effective sorbent material for removing pharmaceuticals, drugs, and their metabolites found in wastewaters. The tested Biochar type was first characterised and used for adsorption experiments of selected micropollutants from a municipal WWTP (wastewater treatment plant) effluent sample. The sorption efficiency was studied on selected pharmaceuticals due to their common presence in aquatic ecosystems. The results show that the studied Biochar type removed the pharmaceuticals with high efficiency (above 90%), so this material can potentially be applied in wastewater treatment. We achieved greater than 99% efficiency in total RNA removal from wastewater. Wastewater might contain infectious RNA fragments of the SARS-CoV-2 virus. However, Biochar can be used as a sorbent in wastewater treatment to remove antibiotic resistance genes. We have also observed a total DNA removal ability of Biochar. On the other hand, the total number and antibiotic-resistant coliform bacteria and enterococci were not changed after Biochar wastewater treatment. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Dosing the Coast: Leaking Sewage Infrastructure Delivers Large Annual Doses and Dynamic Mixtures of Pharmaceuticals to Urban Rivers was written by Fork, Megan L.;Fick, Jerker B.;Reisinger, Alexander J.;Rosi, Emma J.. And the article was included in Environmental Science & Technology in 2021.Category: piperidines The following contents are mentioned in the article:

Pharmaceuticals are commonly detected at low concentrations in surface waters, where they disrupt biol. and ecol. processes. Despite their ubiquity, the annual mass of pharmaceuticals exported from watersheds is rarely quantified. We used liquid chromatog.-mass spectroscopy to screen for 92 pharmaceuticals in weekly samples from an urban stream network in Baltimore, MD, USA, that lacks wastewater treatment effluents. Across the network, we detected 37 unique compounds, with higher concentrations and more compounds in streams with higher population densities. We also used concentrations and stream discharge to calculate annual pharmaceutical loads at the watershed outlet, which range from less than 1 kg to 鈭?5 kg and are equivalent to tens of thousands of human doses. By calculating annual watershed mass balances for eight compounds, we show that 鈭?.05 to 鈭?2% of the pharmaceuticals consumed by humans in this watershed are released to surface waters, with the importance of different pathways (leaking sewage vs treated wastewater effluent) differing among compounds These results demonstrate the importance of developing, maintaining, and improving sewage infrastructure to protect water resources from pharmaceutical contamination. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Category: piperidines).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Screening of pharmaceuticals in coastal waters of the southern coast of Viti Levu in Fiji, South Pacific was written by Dehm, Jasha;Singh, Shubha;Ferreira, Marta;Piovano, Susanna;Fick, Jerker. And the article was included in Chemosphere in 2021.Synthetic Route of C32H39NO4 The following contents are mentioned in the article:

The global reliance on pharmaceuticals coupled with the lack of effective treatment methods has resulted in pseudo-persistence of pharmaceuticals within the environment. Globally, efforts to quantify and monitor pharmaceuticals within the environment have been well underway, however few studies have been made within small Pacific Islands. This study aims at screening for the occurrence and concentration of pharmaceutical residues within the southern coastal waters of Fiji’s main island, Viti Levu. Water samples were collected from a depth of ca. 0.6 m from seven sites and were analyzed for 80 pharmaceuticals via a combination of chromatog. and heated electrospray ionization. Seventy-two pharmaceuticals were quantified at least once with average concentrations ranging between 0.04 ng/L (diltiazem) and 19 ng/L (ketoconazole), and with all but two pharmaceuticals (trimethoprim and biperiden) being present in less than 50% of the samples. Findings suggest that even though the release of pharmaceuticals into the marine environment is sporadic and pharmaceuticals are diluted via turbulent mixing, there are measurable concentrations of pharmaceuticals in Fiji and these pollutants are not necessarily restricted to highly populated areas. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Synthetic Route of C32H39NO4).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Synthetic Route of C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Use of Passive and Grab Sampling and High-Resolution Mass Spectrometry for Non-Targeted Analysis of Emerging Contaminants and Their Semi-Quantification in Water was written by Tadic, Djordje;Manasfi, Rayana;Bertrand, Marine;Sauvetre, Andres;Chiron, Serge. And the article was included in Molecules in 2022.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

Different groups of organic micropollutants including pharmaceuticals and pesticides have emerged in the environment in the last years, resulting in a rise in environmental and human health risks. In order to face up and evaluate these risks, there is an increasing need to assess their occurrence in the environment. Therefore, many studies in the past couple of decades were focused on the improvements in organic micropollutants鈥?extraction efficiency from the different environmental matrixes, as well as their mass spectrometry detection parameters and acquisition modes. This paper presents different sampling methodologies and high-resolution mass spectrometry-based non-target screening workflows for the identification of pharmaceuticals, pesticides, and their transformation products in different kinds of water (domestic wastewater and river water). Identification confidence was increased including retention time prediction in the workflow. The applied methodol., using a passive sampling technique, allowed for the identification of 85 and 47 contaminants in the wastewater effluent and river water, resp. Finally, contaminants鈥?prioritization was performed through semi-quantification in grab samples as a fundamental step for monitoring schemes. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem