1622848-92-3
(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide
CAS: 1622848-92-3
Molecular Formula: C20H19N5O3
1622848-92-3 - Names and Identifiers
1622848-92-3 - Physico-chemical Properties
| Molecular Formula | C20H19N5O3 |
| Molar Mass | 377.4 |
| Density | 1.40±0.1 g/cm3(Predicted) |
| Solubility | DMSO : 100 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound |
| Appearance | solid |
| Color | Off-white |
| pKa | 8.80±0.40(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Use | GSK2982772 is a potent and selective receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate for the Treatment of Inflammatory Diseases. GSK2982772 is, currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis. GSK2982772 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking many TNF-dependent cellular responses. RIP1 has emerged as an important upstream kinase that has been shown to regulate inflammation through both scaffolding and kinase specific functions. |
| Target | human RIP1；monkey RIP1 |
| In vitro study | GSK2982772 has a good active role in the RIP1 cell system, preventing TNF-induced necrotic cell death; In ulcerative colitis explants, it can prevent spontaneous cytokine release. |
| In vivo study | GSK2982772 has nearly equal effect on RIP1 (polarization) of RIP1 of human and monkey origin, but the effect on RIP1 of non primates is significantly reduced, indicating that it is selective for RIP1. GSK2982772 has a good blood free fraction of 4.2% in rats, 11% in dogs, 11% in cynomolgus monkeys, and 7.4% in humans. In rats and monkeys, the inhibitor has a good pharmacokinetic profile. It is widely distributed in a variety of tissues, including the colon, liver, kidney, and heart, and stops at concentrations similar to those in the blood. However, although GSK2982772 has good cell permeability, its brain penetration rate in rats is low (4%), which may be related to the active extrusion of GSK2982772 from the brain by the outflow of drug transporters. GSK2982772 has high oral bioavailability, low to moderate clearance, moderate volume of distribution, and a terminal half-life of about 12 hours. |
1622848-92-3 - Reference
| Reference Show more | [1]. Harris PA, et al. 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. 2017 Feb 23;60(4):1247-1261. |
1622848-92-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.65 ml | 13.249 ml | 26.497 ml |
| 5 mM | 0.53 ml | 2.65 ml | 5.299 ml |
| 10 mM | 0.265 ml | 1.325 ml | 2.65 ml |
| 5 mM | 0.053 ml | 0.265 ml | 0.53 ml |
Last Update：2024-01-02 23:10:35
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Product Name: (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide Visit Supplier Webpage Request for quotationCAS: 1622848-92-3
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Product Name: (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide Visit Supplier Webpage Request for quotationCAS: 1622848-92-3
Tel: 18301782025
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Mobile: 18021002903
QQ: 3008007409
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