[CAS NO. 630103-23-0] MRS2500 tetraammonium
PRODUCTS SPECIFICATIONS [630103-23-0]
DESCRIPTION [630103-23-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 629.28 |
| Molecular Formula | C13H30IN9O8P2 |
| SMILES | O=P(O[C@@H]1[C@]2(COP(O[NH4])(O[NH4])=O)C[C@]2([H])[C@@H](N3C=NC4=C(NC)N=C(I)N=C34)C1)(O[NH4])O[NH4] |
Summary
In Vitro
MRS2500 tetraammonium inhibits platelet aggregation to 10 μM ADP with an IC 50 of 0.95 nM in human washed platelets. MRS2500 tetraammonium inhibits platelet aggregation to 10μM ADP with an IC 50 of 0.49 μM in human PRP [4] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MRS2500 (2 mg/kg; i.v.) decreases acute systemic thromboembolism through selective inhibition of the P2Y1 receptor
[3]
.
MRS2500 exhibited strong antithrombotic efficacy in the prevention of arterial thrombosis in the monkey ECAT model
[4]
..
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 20-25 g WT Male mice (acute vascular occlusion model) [3] |
| Dosage: | 2 mg/kg |
| Administration: | Intravenous |
| Result: | Reduced platelet consumption. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 79.46 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5891 mL | 7.9456 mL | 15.8912 mL |
| 5 mM | 0.3178 mL | 1.5891 mL | 3.1782 mL |
| 10 mM | 0.1589 mL | 0.7946 mL | 1.5891 mL |
References
- [1] Cattaneo M, et al. Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol. 2004;68(10):1995-2002.
- [2] Wong PC, et al. The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys. J Thromb Thrombolysis. 2016;41(3):514-521.
- [3] Hechler B, et al. MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J Pharmacol Exp Ther. 2006;316(2):556