CS-2186
5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide
CAS: 1622849-58-4
Molecular Formula: C21H19N3O4
CS-2186 - Names and Identifiers
CS-2186 - Physico-chemical Properties
| Molecular Formula | C21H19N3O4 |
| Molar Mass | 377.39 |
| Density | 1.35±0.1 g/cm3(Predicted) |
| Boling Point | 677.0±55.0 °C(Predicted) |
| Solubility | DMSO: 30 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 pr |
| pKa | 11.68±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | GSK481 is a Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitor (RIP1 inhibitor). The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to its emergence as a highly promising target for the treatment of multiple inflammatory diseases. |
| Target | RIP1 |
| In vitro study | GSK481 can inhibit the phosphorylation of human and mouse RIP1(WT)S166, which is overexpressed in HEK293T cells. The inhibitory effect of GSK481 on human and cynomolgus RIP1 is almost the same, but the efficacy of RIP on non-primate is much worse. |
CS-2186 - Reference
| Reference Show more | 1: Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA,Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J,Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS,Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, ZhangA, Zhang D, Marquis RW, Bertin J, Gough PJ. DNA-Encoded Library ScreeningIdentifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and MonoselectiveReceptor Interacting Protein 1 Kinase Inhibitors. J Med Chem. 2016 Mar10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. PubMed PMID: 26854747. |
CS-2186 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.65 ml | 13.249 ml | 26.498 ml |
| 5 mM | 0.53 ml | 2.65 ml | 5.3 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
CS-2186 - Reference Information
| biological activity | GSK481 is an inhibitor of RIP1(Receptor Interacting Protein Kinase1, RIPK1), which inhibits RIP1 to hinder cell necrosis. |
| target | TargetValue RIP1 |
| Target | Value | in vitro study | GSK481 can inhibit the phosphorylation of human and mouse RIP1(WT)S166 overexpressed in HEK293T cells. GSK481 has almost the same inhibitory effect on human and cynomolgus monkey RIP1, but it is much less effective on non-primate RIP. |
Last Update：2024-04-09 21:54:55
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Multiple SpecificationsSpot supply
Product Name: GSK481 (Standard) Visit Supplier Webpage Request for quotationCAS: 1622849-58-4
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
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Product Name: GSK'481 Visit Supplier Webpage Request for quotationCAS: 1622849-58-4
Tel: +86-400-900-4166
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Mobile: +86-18621343501
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Product Name: 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide Visit Supplier Webpage Request for quotationCAS: 1622849-58-4
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