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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G414024-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $195.90 | |
G414024-10mg | 10mg | In stock | $303.90 | |
G414024-25mg | 25mg | In stock | $684.90 | |
G414024-50mg | 50mg | In stock | $913.90 | |
G414024-100mg | 100mg | In stock | $1,360.90 |
RIP kinase Inhibitors
Synonyms | GSK2982772|1622848-92-3|GSK-2982772|(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|(S)-3-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-5-carboxamide|T |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of receptor interacting serine/threonine kinase 1 |
Product Description | Information GSK2982772 GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses. Targets human RIP1 (Cell-free assay) 16 nM In vitro GSK2982772 has excellent activity in both RIP1 cellular systems, preventing TNF induced necrotic cell death, and an ulcerative colitis explant assay blocking spontaneous cytokine release. In vivo GSK2982772 exhibits approximately equivalent RIP1 FP potency against human and monkey RIP1 but was significantly less potent against nonprimate RIP1. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, it has low brain penetration in rat (4%) despite possessing good cell permeability, which is likely due to active extrusion of GSK2982772 from the brain via the efflux drug transporter. It is predicted that GSK2982772 has high bioavailability, moderate to low clearance with a moderate volume, and a terminal half-life in the order of 12 h. |
ALogP | 1.639 |
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HBD Count | 2 |
Rotatable Bond | 4 |
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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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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 |
InChi Key | LYPAFUINURXJSG-AWEZNQCLSA-N |
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 |
Alternate CAS | 1622848-92-3 |
PubChem CID | 77108121 |
MeSH Entry Terms | 1H-1,2,4-Triazole-5-carboxamide, 3-(phenylmethyl)-N-((3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl)-;3-Benzyl-N-((3S)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepin-3-yl)-1H-1,2,4-triazole-5-carboxamide;GSK2982772 |
Molecular Weight | 377.4 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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I2207714 | Certificate of Analysis | Jun 17, 2022 | G414024 |
I2207715 | Certificate of Analysis | Jun 17, 2022 | G414024 |
I2207716 | Certificate of Analysis | Jun 17, 2022 | G414024 |
I2207717 | Certificate of Analysis | Jun 17, 2022 | G414024 |
Solubility | Solubility (25°C) In vitro DMSO: 75 mg/mL (198.72 mM); Ethanol: 30 mg/mL (79.49 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 75 |
DMSO(mM) Max Solubility | 198.7281399 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X et al.. (2017) Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.. J Med Chem, 60 (4): (1247-1261). [PMID:28151659] |