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PAR4 antagonist
BMS-986120 是一种首创的口服可逆性蛋白酶激活受体4(PAR4)拮抗剂,其在人类和猴子血液中的半抑制浓度(IC50)分别为9.5 nM和2.1 nM。 -
PAR-1 Antagonist
Vorapaxar (SCH 530348) 是一种强效且可口服的凝血酶受体(PAR-1)拮抗剂,其Ki值为8.1 nM。- Arundhasa Chandrabalan, .et al. , Am J Physiol Cell Physiol, 2023, Jul 1;325(1):C272-C285 PMID: 37273236
- Arundhasa Chandrabalan, .et al. , Sci Rep, 2023, Jan 20;13(1):1124 PMID: 36670151
- Cansu Tekin, .et al. , Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. , Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. , J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. , Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. , J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. , Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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PAR4 antagonist
UDM-001651 是一种强效、选择性且可口服活性的蛋白酶激活受体4(PAR4)拮抗剂,具有体内抗血栓效力(IC50 = 2.4 nM)。