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AB286962

GSK-2982772

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(1 Publication)

MW 377.4 Da, Purity >98%. A potent and ATP-competitive receptor-interacting protein-1 (RIP1) kinase inhibitor (IC50 = 1 nM).

View Alternative Names

(R)-limonene 6-monooxygenase, (S)-limonene 6-monooxygenase, (S)-limonene 7-monooxygenase, BXR, CP2C9_HUMAN, CPC9, CYP2C, CYP2C10, CYPIIC9, Cell death protein RIP, Cytochrome P-450MP, Cytochrome P450 2C9, Cytochrome P450 MP-4, Cytochrome P450 MP-8, Cytochrome P450 PB-1, Cytochrome P450, family 2, subfamily C, polypeptide 9, FLJ39204, MGC149605, MGC88320, Microsomal monooxygenase, NR1I2_HUMAN, Nuclear receptor subfamily 1 group I member 2, ONR 1, OTTHUMP00000020135, OTTHUMP00000039163, OTTHUMP00000215173, OTTHUMP00000215174, OTTHUMP00000215175, Orphan nuclear receptor PAR 1, Orphan nuclear receptor PXR, P450 MP, P450 PB 1, P450IIC9, PAR, PAR q, PRR, Pregnane X receptor, RIPK1_HUMAN, Receptor (TNFRSF) interacting serine threonine kinase 1, Receptor TNFRSF interacting serine threonine kinase 1, Receptor interacting protein, Receptor interacting protein kinase 1, Receptor interacting serine threonine protein kinase 1, Receptor-interacting protein 1, Receptor-interacting serine/threonine-protein kinase 1, Rinp, Rip-1, S-mephenytoin 4-hydroxylase, SXR, Serine threonine protein kinase RIP, Serine/threonine-protein kinase RIP, Steroid and xenobiotic receptor, Xenobiotic monooxygenase, cytochrome P-450 S-mephenytoin 4-hydroxylase, flavoprotein-linked monooxygenase, pregnane X nuclear receptor variant 2

Key facts

CAS number

1622848-92-3

Purity

>98%

Form

Solid

form

Molecular weight

377.4 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>1</sub><sub>9</sub>N<sub>5</sub>O<sub>3</sub>

PubChem

77108121

Nature

Synthetic

Solubility

Soluble in DMSO

Biochemical name

(S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-3-carboxamide

Biological description

A potent and ATP-competitive receptor-interacting protein-1 (RIP1) kinase inhibitor (IC50 = 1 nM).

Canonical smiles

CN1C2=CC=CC=C2OCC(C1=O)NC(=O)C3=NNC(=N3)CC4=CC=CC=C4

Isomeric smiles

CN1C2=CC=CC=C2OC[C@@H](C1=O)NC(=O)C3=NNC(=N3)CC4=CC=CC=C4

InChi

InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1

InChiKey

LYPAFUINURXJSG-AWEZNQCLSA-N

IUPAC Name

5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2232 GSK-2982772. B2232-5 is the same size as the 5 mg size of ab286962.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark|Store under desiccating conditions|This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The CYP2C9 protein also known as Cytochrome P450 2C9 is a part of the cytochrome P450 family. It has a molecular mass of approximately 55 kDa. This enzyme is highly expressed in the liver and plays an important role in metabolizing a variety of endogenous compounds and xenobiotics. CYP2C9 is involved in oxidative reactions where it catalyzes the insertion of oxygen into organic substrates through electron transfer processes facilitated by heme as a prosthetic group.
Biological function summary

CYP2C9 participates in the metabolism of several drugs like warfarin and phenytoin rendering them into more water-soluble forms for excretion. This enzyme also contributes to the bioactivation of certain pro-drugs. CYP2C9 does not work alone; it often functions as part of a protein complex with other proteins in the endoplasmic reticulum membrane playing an important role in phase I drug metabolism.

Pathways

CYP2C9 is involved significantly in metabolic pathways including the drug metabolism-cytochrome P450 pathway and the arachidonic acid metabolism pathway. It relates closely to other enzymes in the cytochrome P450 family such as CYP2C19 and CYP2C8 due to overlapping substrate specificities and regulatory mechanisms. These enzymes work together to ensure proper metabolic processing of a wide range of substances.

Genetic variations in CYP2C9 are well-linked with altered drug metabolism leading to conditions such as warfarin sensitivity and phenytoin toxicity. Individuals with certain polymorphisms in this gene may experience unusual drug effects or adverse reactions. Additionally CYP2C9 polymorphisms connect with VKORC1 (Vitamin K epoxide reductase complex subunit 1) in affecting drug dosage requirements for anticoagulant therapy.
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Product protocols

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Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Journal of medicinal chemistry 60:1247-1261 PubMed28151659

2017

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Applications

Unspecified application

Species

Unspecified reactive species

Philip A Harris,Scott B Berger,Jae U Jeong,Rakesh Nagilla,Deepak Bandyopadhyay,Nino Campobasso,Carol A Capriotti,Julie A Cox,Lauren Dare,Xiaoyang Dong,Patrick M Eidam,Joshua N Finger,Sandra J Hoffman,James Kang,Viera Kasparcova,Bryan W King,Ruth Lehr,Yunfeng Lan,Lara K Leister,John D Lich,Thomas T MacDonald,Nathan A Miller,Michael T Ouellette,Christina S Pao,Attiq Rahman,Michael A Reilly,Alan R Rendina,Elizabeth J Rivera,Michelle C Schaeffer,Clark A Sehon,Robert R Singhaus,Helen H Sun,Barbara A Swift,Rachel D Totoritis,Anna Vossenkämper,Paris Ward,David D Wisnoski,Daohua Zhang,Robert W Marquis,Peter J Gough,John Bertin
View all publications
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Complementary Products

Secondary Antibodies

AB150113

Goat Anti-Mouse IgG H&L (Alexa Fluor® 488)

Immunocytochemistry/ Immunofluorescence - Goat Anti-Mouse IgG H&L (Alexa Fluor® 488) (AB150113)

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Primary Antibodies

AB192579

Anti-PXR antibody

Western blot - Anti-PXR antibody (AB192579)

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Secondary Antibodies

AB172329

Rat monoclonal [SB76b] Anti-Mouse IgG3 gamma chain (Alexa Fluor® 647)

Flow Cytometry - Rat monoclonal [SB76b] Anti-Mouse IgG3 gamma chain (Alexa Fluor® 647) (AB172329)

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Proteins & Peptides

AB7403

Streptavidin (HRP)

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Streptavidin (HRP) (AB7403)

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