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ChemicalBook--->CAS DataBase List--->1478712-37-6

1478712-37-6

1478712-37-6 Structure

1478712-37-6 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS05,GHS08,GHS07
[Signal word ]

Danger
[Hazard statements ]

H315-H318-H334-H317-H341-H361-H370-H335-H413
[Precautionary statements ]

P201-P202-P260-P264-P270-P272-P273-P280-P284-P302+P352-P304+P341-P305+P351+P338-P310-P308+P313-P321-P362+P364-P333+P313-P342+P311-P363-P405-P501
Hazard InformationBack 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
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