| 产品描述: | Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo |
| 靶点: |
IC50: 0.26 μM (PAR1);Protease-activatedReceptor |
| 体内研究: |
Parmodulin 2 (ML161; 5 mg/kg; IV) significantly inhibits platelet thrombus formation, with a 73% inhibition in AUC (area under the curve).Parmodulin 2 inhibits platelet thrombus formation in vivo, and it does not prolong bleeding time. Parmodulin 2 selectively inhibits platelet aggregation through Par1 and the α2A-adrenergic receptor. Animal Model: C57BL/6J wild type mice Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Significantly inhibited platelet thrombus formation, with a 73% inhibition in AUC. |
| 参考文献: |
1. Gandhi DM, et al. Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. Bioorg Med Chem. 2018 May 15;26(9):2514-2529. 2. Susanna F Gunnink, et al. Allosteric inhibition of protease activated receptor 1: a new antiplatelet therapy. 3. Aisiku O, et al. Parmodulins inhibit thrombus formation without inducing endothelial injury caused by vorapaxar. Blood. 2015 Mar 19;125(12):1976-85. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.768 ml |
13.842 ml |
27.683 ml |
| 5 mM |
0.554 ml |
2.768 ml |
5.537 ml |
| 10 mM |
0.277 ml |
1.384 ml |
2.768 ml |
| 50 mM |
0.055 ml |
0.277 ml |
0.554 ml |
|
| 注意: |
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