Day: November 24, 2022

A HaloTag-Based Small Molecule Microarray Screening Methodology with Increased Sensitivity and Multiplex Capabilities was written by Noblin, Devin J.;Page, Charlotte M.;Tae, Hyun Seop;Gareiss, Peter C.;Schneekloth, John S.;Crews, Craig M.. And the article was included in ACS Chemical Biology in 2012.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Small Mol. Microarrays (SMMs) represent a general platform for screening small mol.-protein interactions independent of functional inhibition of target proteins. In an effort to increase the scope and utility of SMMs, the authors have modified the SMM screening methodol. to increase assay sensitivity and facilitate multiplex screening. Fusing target proteins to the HaloTag protein allows the authors to covalently prelabel fusion proteins with fluorophores, leading to increased assay sensitivity and an ability to conduct multiplex screens. The authors use the interaction between FKBP12 and two ligands, rapamycin and ARIAD’s bump ligand, to show that the HaloTag-based SMM screening methodol. significantly increases assay sensitivity. Addnl., using wild type FKBP12 and the FKBP12 F36V mutant, prelabeling various protein isoforms with different fluorophores allows the authors to conduct multiplex screens and identify ligands to a specific isoform. Finally, the authors show this multiplex screening technique is capable of identifying ligands selective for a specific PTP1B isoform using a 20,000-compound screening deck. 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. 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.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sediment-Water Distribution and Benthic Boundary Layer Fluxes of Pharmaceuticals and Personal Care Products near Wastewater Discharge into a Tidal River Shoal was written by Foster, Gregory D.;Leahigh, Arion. And the article was included in ACS ES&T Water in 2021.Formula: C32H39NO4 The following contents are mentioned in the article:

Pharmaceuticals and personal care products (PPCPs) were measured in porewater, sediment, and surface water at three sites near wastewater treatment plant (WTP) discharge along a 2 km downstream transect in a tributary shoal embayment (Alexandria, VA) of the tidal Potomac River. A benthic diffusion layer model evaluated water-only, dissolved organic carbon (DOC)-associated, and bioturbation mass transport pathways. Fluxes of 17 PPCPs nearest the WTP were all in the direction of surface water to sediment porewater (neg.) with magnitudes of -0.0016 to -7.4 ng m-2 s-1. At the next downstream site, fluxes of seven PPCPs were bidirectional (neg. and pos.) and ranged from -4.8 x 10-4 to 0.0051 ng m-2 s-1. The furthest site downstream yielded fluxes of six PPCPs that were predominantly sediment to water (pos.), ranging in magnitude from -0.0020 to 7.0 x 10-4 ng m-2 s-1. The bioturbation and water-only mass transport coefficients contributed most to fluxes for PPCPs. The DOC-associated mass transport term was negligible. The fluxes indicated sediments will continue serve as a source of PPCPs 2 km downstream from WTP discharge. 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: 83799-24-0Formula: 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 is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Formula: C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Mosquito saliva enhances virus infection through sialokinin-dependent vascular leakage was written by Lefteri, Daniella A.;Bryden, Steven R.;Pingen, Marieke;Terry, Sandra;McCafferty, Ailish;Beswick, Emily F.;Georgiev, Georgi;Van der Laan, Marleen;Mastrullo, Valeria;Campagnolo, Paola;Waterhouse, Robert M.;Varjak, Margus;Merits, Andres;Fragkoudis, Rennos;Griffin, Stephen;Shams, Kave;Pondeville, Emilie;McKimmie, Clive S.. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2022.Product Details of 83799-24-0 The following contents are mentioned in the article:

Viruses transmitted by Aedes mosquitoes are an increasingly important global cause of disease. Defining common determinants of host susceptibility to this large group of heterogenous pathogens is key for informing the rational design of panviral medicines. Infection of the vertebrate host with these viruses is enhanced by mosquito saliva, a complex mixture of salivary-gland-derived factors and microbiota. We show that the enhancement of infection by saliva was dependent on vascular function and was independent of most antisaliva immune responses, including salivary microbiota. Instead, the Aedes gene product sialokinin mediated the enhancement of virus infection through a rapid reduction in endothelial barrier integrity. Sialokinin is unique within the insect world as having a vertebrate-like tachykinin sequence and is absent from Anopheles mosquitoes, which are incompetent for most arthropod-borne viruses, whose saliva was not proviral and did not induce similar vascular permeability. Therapeutic strategies targeting sialokinin have the potential to limit disease severity following infection with Aedes-mosquito-borne viruses. 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: 83799-24-0Product Details of 83799-24-0).

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 derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Product Details of 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Targeting spinal microglia with fexofenadine-loaded nanoparticles prolongs pain relief in a rat model of neuropathic pain was written by Tran, Quangdon;Pham, Thuy Linh;Shin, Hyo Jung;Shin, Juhee;Shin, Nara;Kwon, Hyeok Hee;Park, Hyewon;Kim, Song I.;Choi, Seoung Gyu;Wu, Junhua;Ngo, Van T. H.;Park, Jin Bong;Kim, Dong Woon. And the article was included in Nanomedicine (New York, NY, United States) in 2022.Synthetic Route of C32H39NO4 The following contents are mentioned in the article:

Targeting microglial activation is emerging as a clin. promising drug target for neuropathic pain treatment. Fexofenadine, a histamine receptor 1 antagonist, is a clin. drug for the management of allergic reactions as well as pain and inflammation. However, the effect of fexofenadine on microglial activation and pain behaviors remains elucidated. Here, we investigated nanomedicinal approach that targets more preferentially microglia and long-term analgesics. Fexofenadine significantly abolished histamine-induced microglial activation. The fexofenadine-encapsulated poly(lactic-co-glycolic acid) nanoparticles (Fexo NPs) injection reduced the pain sensitivity of spinal nerve ligation rats in a dose-dependent manner. This alleviation was sustained for 4 days, whereas the effective period by direct fexofenadine injection was 3 h. Moreover, Fexo NPs inhibited microglial activation, inflammatory signaling, cytokine release, and a macrophage phenotype shift towards the alternative activated state in the spinal cord. These results show that Fexo NPs exhibit drug repositioning promise as a long-term treatment modality for neuropathic pain. 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. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Synthetic Route of C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Effects of Osthole on Inflammatory Gene Expression and Cytokine Secretion in Histamine-Induced Inflammation in the Caco-2 Cell Line was written by Kordulewska, Natalia K.;Topa, Justyna;Rozmus, Dominika;Jarmolowska, Beata. And the article was included in International Journal of Molecular Sciences in 2021.Product Details of 83799-24-0 The following contents are mentioned in the article:

Hyperactivity of the immune system in the gastrointestinal tract leads to the development of chronic, inflammation-associated disorders. Such diseases, including inflammatory bowel disease, are not completely curable, but the specific line of treatment may reduce its symptoms. However, the response to treatment varies among patients, creating a necessity to uncover the pathophysiol. basis of immune-mediated diseases and apply novel therapeutic strategies. The present study describes the anti-inflammatory properties of osthole during histamine-induced inflammation in the intestinal Caco-2 cell line. Osthole reduced the secretion of cytokines (CKs) and the expression level of inflammation-associated genes, which were increased after a histamine treatment. We have shown that the secretion of pro-inflammatory CKs (IL-1尾, IL-6, IL-8, and TNF-伪) during inflammation may be mediated by NF魏B, and, after osthole treatment, this signaling pathway was disrupted. Our results suggest a possible role for osthole in the protection against inflammation in the gastrointestinal tract; thus, osthole may be considered as an anti-inflammatory modulator. 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: 83799-24-0Product Details of 83799-24-0).

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 are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Product Details of 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Stability indicating method development and validation for the simultaneous estimation of fexofenadine and Montelukast by using RP-UPLC was written by Jaldi, Christina Emette;Kuna, Mangamma. And the article was included in International Journal of Pharmaceutical Sciences and Research in 2021.Product Details of 83799-24-0 The following contents are mentioned in the article:

A simple, reliable, accurate, and precise method was developed for the simultaneous estimation of Fexofenadine and Montelukast in pharmaceutical dosage form. The chromatogram was run through Standard HSS C18 (2.1 x 100 mm, 1.8渭m). Mobile phase employed was 0.1% OPA Buffer and Acetonitrile taken in the ratio of 65:35 was pumped through column at a flow rate of 0.2 mL/min. The temperature was maintained at 30掳C. The optimized wavelength selected was 269 nm. The retention time of Montelukast and Fexofenadine was found to be 0.921 and 1.101 min. The Percent RSD of the Montelukast and Fexofenadine were and found to be 0.7% and 0.4% resp. The Percent recovery was obtained as 99.22% and 99.67% for Montelukast and Fexofenadine resp. The LOD and LOQ values obtained from regression equations of Montelukast and Fexofenadine were 0.06, 0.18 and 0.80, 2.44 resp. Regression equation of Montelukast was y = 6333.8x + 755.96 and y = 4038.3x + 8964.8 of Fexofenadine. The decrease in the retention and run times in this method that has been developed was simple and economical that can be been easily adopted in regular quality control test in industries. 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: 83799-24-0Product Details of 83799-24-0).

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 metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Product Details of 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Novel bovine serum album and 尾-cyclodextrin-based mixed chiral stationary phase for the enantioseparation in capillary electrochromatography was written by Tang, Weiyang;Lu, Yao;Row, Kyung Ho;Baeck, Sung Hyeon;Zhang, Yifan;Sun, Genlin. And the article was included in Microchemical Journal in 2022.HPLC of Formula: 83799-24-0 The following contents are mentioned in the article:

A capillary was co-immobilized with mixed 尾-cyclodextrin and bovine serum album by chem. covalent coupling as the chiral stationary phase for the enantioseparation of proton-pump inhibitors in capillary electrochromatog. The chromatog. parameters including buffer concentration, pH value, organic modifier, and applied voltage were optimized. The separation performance of the developed column was evaluated by enantiosepg. omeprazole, lansoprazole, pantoprazole, and esomeprazole with extremely high resolutions of 5.21, 7.11, 6.39, and 4.75, resp. Moreover, the mixed chiral stationary phase exhibited a broader range and could sep. more than 10 chiral analytes compared to the single-selector column. The relative standard deviations of the day-to-day and column-to-column repeatability were less than 4%, demonstrating excellent stability of the fabricated column. An open tubular capillary immobilized with the bovine serum album and 尾-cyclodextrin as the chiral stationary phase is a promising prospect for separating chiral drugs in capillary electrochromatog. because of the combination of the enantioselectivities of both individual selectors. 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: 83799-24-0HPLC of Formula: 83799-24-0).

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. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.HPLC of Formula: 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Isolation of MDCK cells with low expression of mdr1 gene and their use in membrane permeability screening was written by Bokulic, Ana;Padovan, Jasna;STUPIN-POLANCEC, Darija;Milic, Astrid. And the article was included in Acta Pharmaceutica (Warsaw, Poland) in 2022.Computed Properties of C32H39NO4 The following contents are mentioned in the article:

The Madin-Darby canine kidney (MDCK) cell line is frequently used for permeability screening in drug discovery. It contains endogenous transporters, most prominently canine multidrug resistance P-glycoprotein (Mdr1), which can interfere with studies of P-glycoprotein substrate assessment and permeability measurements. Because MDCK wild type (WT) is genetically heterogeneous, an isolation procedure was investigated in this study to obtain the subclonal line with low P-glycoprotein expression. The best clone obtained had up to 3-fold lower amprenavir efflux and P-glycoprotein expression in comparison to WT. Of 12 standard compounds tested that exhibited active efflux in WT cells, 11 showed a decrease in efflux in the isolated clone. However, the decrease was not below the cut-off value of 2, indicating residual P–glycoprotein activity. Clone isolation via the limiting dilution method, combined with bidirectional amprenavir permeability for clone selection, successfully identified MDCK clones with substantially lower P-glycoprotein efflux and has been demonstrated as a useful tool for assessing passive permeability in early drug discovery. 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: 83799-24-0Computed Properties 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 and its derivatives have become increasingly popular in many synthetic schemes. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Computed Properties of C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Biological activity of endomorphin and [Dmt¹]endomorphin analogs with six-membered proline surrogates in position 2 was written by Perlikowska, Renata;Gach, Katarzyna;Fichna, Jakub;Toth, Geza;Walkowiak, Bogdan;do-Rego, Jean-Claude;Janecka, Anna. And the article was included in Bioorganic & Medicinal Chemistry in 2009.Quality Control of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Endogenous 渭-opioid receptor (MOR) selective peptides, endomorphin-1 (EM-1) and endomorphin-2 (EM-2), unlike so called typical opioids’, are characterized by the presence of Pro² residue, which is a spacer connecting aromatic pharmacophoric residues. In order to investigate structural requirements for position 2, we synthesized endomorphin analogs incorporating, instead of Pro, unnatural amino acids with six-membered heterocyclic rings, such as piperidine 2-, 3- or 4-carboxylic acids (Pip, Nip and Inp, resp.). (R)-Nip residue turned out to be favorable for improving MOR affinity. Introduction of 2′,6′-dimethyltyrosine (Dmt) instead of Tyr¹ led to obtaining [Dmt¹, (R)-Nip²]EM-2 which showed exceptional MOR affinity and high stability against enzymic degradation in rat brain homogenate. In in vivo hot-plate test in mice, this analog given intracerebroventricularly (i.c.v.), produced profound supraspinal analgesia, being much more potent than EM-2. The antinociceptive effect of this analog lasted about 170 min and was almost completely reversed by 尾-funaltrexamine (尾-FNA), a selective MOR antagonist. 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. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Quality Control of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Biological activity of endomorphin and [Dmt¹]endomorphin analogs with six-membered proline surrogates in position 2 was written by Perlikowska, Renata;Gach, Katarzyna;Fichna, Jakub;Toth, Geza;Walkowiak, Bogdan;do-Rego, Jean-Claude;Janecka, Anna. And the article was included in Bioorganic & Medicinal Chemistry in 2009.HPLC of Formula: 86069-86-5 The following contents are mentioned in the article:

Endogenous 渭-opioid receptor (MOR) selective peptides, endomorphin-1 (EM-1) and endomorphin-2 (EM-2), unlike so called typical opioids’, are characterized by the presence of Pro² residue, which is a spacer connecting aromatic pharmacophoric residues. In order to investigate structural requirements for position 2, we synthesized endomorphin analogs incorporating, instead of Pro, unnatural amino acids with six-membered heterocyclic rings, such as piperidine 2-, 3- or 4-carboxylic acids (Pip, Nip and Inp, resp.). (R)-Nip residue turned out to be favorable for improving MOR affinity. Introduction of 2′,6′-dimethyltyrosine (Dmt) instead of Tyr¹ led to obtaining [Dmt¹, (R)-Nip²]EM-2 which showed exceptional MOR affinity and high stability against enzymic degradation in rat brain homogenate. In in vivo hot-plate test in mice, this analog given intracerebroventricularly (i.c.v.), produced profound supraspinal analgesia, being much more potent than EM-2. The antinociceptive effect of this analog lasted about 170 min and was almost completely reversed by 尾-funaltrexamine (尾-FNA), a selective MOR antagonist. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5HPLC of Formula: 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 structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.HPLC of Formula: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem