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BMS-986120
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-986120图片
CAS NO:1478712-37-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
理化性质和储存条件


Name: BMS-986120
CAS#: 1478712-37-6
Chemical Formula: C23H23N5O5S2
Exact Mass: 513.1141
Molecular Weight: 513.587
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationSynonym: BMS 986120; BMS-986120; BMS986120.
Chemical Name: 4-(4-(((6-methoxy-2-(2-methoxyimidazo[2,1-b][1,3,4]thiadiazol-6-yl)benzofuran-4-yl)oxy)methyl)-5-methylthiazol-2-yl)morpholine
InChi Key: MINMDCMSHDBHKG-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H23N5O5S2/c1-13-17(25-21(34-13)27-4-6-31-7-5-27)12-32-18-8-14(29-2)9-19-15(18)10-20(33-19)16-11-28-22(24-16)35-23(26-28)30-3/h8-11H,4-7,12H2,1-3H3
SMILES Code: COC1=NN2C(S1)=NC(C(O3)=CC4=C3C=C(OC)C=C4OCC(N=C5N6CCOCC6)=C(S5)C)=C2
实验参考方法
Target

IC50: 9.5 (PAR4, human), 2.1 nM (PAR4, monkey)[1].

In VitroBMS-986120 (BMS) comparably inhibits PA induced by PAR4-AP in human and monkey blood in vitro (IC50 of 9.5±2.7 and 2.1±0.4 nM, respectively)[1].
In VivoIn monkeys, BMS-986120 produces parallel rightward shifts in the log PA dose response to PAR4-AP without affecting maximum response, suggesting surmountable antagonism. BMS (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. BMS (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. A maximum antiplatelet dose of ASA (4 mg/kg/h, n=8) slightly reduces TW by 12±2% and increases KBT and MBT by 2.2- and 2.7-fold, respectively. Co-administration of ASA and BMS (0.5 or 1 mg/kg) reduce TW by 54±3 and 95±2%, increase KBT by 3.1- and 3.6-fold, and increase MBT by 2.6- and 3.3-fold, respectively (n=8/group). In companion monkey studies, clopidogrel (0.3 mg/kg/day, n=6) alone reduces TW by 49±6%, but increases KBT and MBT by 7.3- and 8.1-fold, respectively[1].
Animal AdminMonkeys[1] Individual anesthetized monkeys are given orally of BMS-986120 (BMS: 0.2, 0.5,1 mg/kg) or vehicle (n=8/group) 2 hour before a combination of thrombosis, BT and ex vivo biomarker experiments. Aspirin alone (ASA, 4 mg/kg/h IV) or in combination with BMS-986120 (0.5, 1 mg/kg) is also studied (n=8/group). Thrombus weight (TW) reduction, BT increase over vehicle in kidney (KBT) and mesenteric artery (MBT), and platelet aggregation (PA) inhibition are determined. Peak PA responses to activation peptides selective for PAR4 (PAR4-AP, 12.5 μM) and PAR1 (PAR1-AP, 18 μM), ADP (20 μM), and collagen (5 μg/mL) are determined by whole blood aggregometry[1].
References

[1]. 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.