ML-161 is an allosteric and reversible inhibitor of proteinase-activated receptor 1 (PAR1) with IC50 of 0.26 μM.
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描述 | Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1), with an IC50 of 0.26 μM [1]. Parmodulin 2 effectively inhibits SFLLRN-induced P-selectin expression, thereby suppressing platelet aggregation in vitro and platelet thrombus formation in vivo[2]. |
体内研究 | Parmodulin 2 (ML161; 5 mg/kg; administered intravenously) significantly inhibits platelet thrombus formation, resulting in a 73% reduction in AUC [2]. Parmodulin 2 inhibits platelet thrombus formationin vivowithout prolonging bleeding time. It selectively inhibits platelet aggregation through PAR1 and the α2A-adrenergic receptor [2]. |
体外研究 | Parmodulin 2 (ML161; at a concentration of 10 µM for 30 minutes) suppresses proinflammatory signaling in endothelial HUVECs cells [3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.84mL 2.77mL 1.38mL |
27.68mL 5.54mL 2.77mL |
CAS号 | 423735-93-7 |
分子式 | C17H17BrN2O2 |
分子量 | 361.233 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(290.67 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |