ML-161 is a potent and reversible inhibitor of proteinase-activated receptor 1 (PAR1) on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 µM. ML161 inhibited platelet aggregation induced by a PAR1 peptide agonist or by thrombin but not by several other platelet agonists. Initial studies suggest that ML161 is an allosteric inhibitor of PAR1. These findings may be important for the discovery of antithrombotics with an improved safety profile.
MedKoo Cat#: 530449
Name: ML161
CAS#: 423735-93-7
Chemical Formula: C17H17BrN2O2
Exact Mass: 360.0473
Molecular Weight: 361.24
Elemental Analysis: C, 56.52; H, 4.74; Br, 22.12; N, 7.75; O, 8.86
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 44.4 | 122.84 | ||
| Ethanol | 30.6 | 84.60 |
The following data is based on the product molecular weight 361.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
