2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. BMS-986141

BMS-98614 是一种口服活性的、选择性的凝血酶受体蛋白酶激活受体-4 (PAR-4) (protease-activated receptor-4 (PAR-4)) 拮抗剂，其 IC50 值为 0.4 nM。BMS-98614 具有优异的抗血栓功效。

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BMS-986141 Chemical Structure

BMS-986141 Chemical Structure

CAS No. : 1478711-48-6

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BMS-986141 相关抗体

Top Publications Citing Use of Products

查看 Protease Activated Receptor (PAR) 亚型特异性产品:

查看所有亚型
PAR1 PAR2 PAR4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect[1][2].

IC50 & Target[1]

PAR4

.4 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Platelet IC50
2.1 nM
Compound: 49; BMS-986141
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
[PMID: 35729784]
体外研究
(In Vitro)

BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986141 相关抗体:
体内研究
(In Vivo)

BMS-986141 (compound 49) shows a slight but significant prolongation of KBT (kidney bleeding time) and demonstrates excellent anti-thrombotic efficacy at 0.5 mg/kg in cynomolgus monkey[1][2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models[2]
Dosage: 0.05, 0.1, 0.5 mg/kg
Administration: p.o., 2 hours
Result: Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively.
Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model.
Increased MBT by 1.2 times.
Animal Model: Rat, dog and monkey[1]
Dosage: 0.5, 1, 2 mpk
Administration: i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey
Result: The pharmacokinetic parameters of BMS-986141 (compound 49)
Parameters rat dog monkey
t1/2(h) 3.7 ± 0.4 13 75 ± 12
CL (mL/min/kg) 14.3 ± 0.4 8.5 12 ± 2
Vss(L/kg) 2.7 ± 0.3 2.7 14 ± 5
F (%) 31 25 36
Clinical Trial
分子量

561.63

Formula

C27H23N5O5S2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

BMS-986141 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

BMS-9861411478711-48-6BMS986141BMS 986141Protease Activated Receptor (PAR)Thrombin receptorsplatelet thrombin receptorantagonistPAR4protease-activated receptor-4antithromboticInhibitorinhibitorinhibit

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目录号：
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