| Identification | Back Directory | [Name]
BMS-986120 | [CAS]
1478712-37-6 | [Synonyms]
BMS-986120
BMS-986120 1478712-37-6
2-methoxy-6-[6-methoxy-4-[[5-methyl-2-(4-morpholinyl)-4-thiazolyl]methoxy]-2-benzofuranyl]-imidazo[2,1-b]-1,3,4-thiadiazole
Imidazo[2,1-b]-1,3,4-thiadiazole, 2-methoxy-6-[6-methoxy-4-[[5-methyl-2-(4-morpholinyl)-4-thiazolyl]methoxy]-2-benzofuranyl]- | [Molecular Formula]
C23H23N5O5S2 | [MDL Number]
MFCD30532696 | [MOL File]
1478712-37-6.mol | [Molecular Weight]
513.59 |
| Chemical Properties | Back Directory | [density ]
1.57±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
A crystalline solid | [pka]
4.87±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects[1][2]. | [in vivo]
In monkeys, BMS-986120 (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. BMS-986120 (0.2, 0.5, 1 mg/kg) reduces TW by 35±5, 49±4, and 83±4%, respectively. Maximum KBT and MBT increases are only 2.2-fold and 1.8-fold, respectively[1]. | [IC 50]
PAR1; PAR4 | [References]
[1] Pancras C Wong, et al. Abstract 175: A Novel Orally-Active Small-Molecule Antagonist of the Platelet Protease-Activated Receptor-4, BMS-986120, Inhibits Arterial Thrombosis With Limited Impact on Hemostasis in Cynomolgus Monkeys. Stroke. 2018;47:A175.
[2] Wilson SJ, et al. PAR4 (Protease-Activated Receptor 4) Antagonism With BMS-986120 Inhibits Human Ex VivoThrombus Formation. Arterioscler Thromb Vasc Biol. 2018 Feb;38(2):448-456. DOI:10.1161/ATVBAHA.117.310104
[3] Wong PC, et al. Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding. Sci Transl Med. 2017 Jan 4;9(371). DOI:10.1126/scitranslmed.aaf5294 |
|
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|