CAS NO: | 145782-74-7 |
包装: | 1mg |
市场价: | 4988元 |
Cas No. | 145782-74-7 |
Canonical SMILES | CCCSC1=NC(N)=C(N=CN2[C@@]3([H])[C@](O)([H])[C@@](O)([H])[C@@](O3)([H])COP([O-])(OP(C(F)(P([O-])([O-])=O)F)([O-])=O)=O)C2=N1.[Na+].[Na+].[Na+].[Na+] |
分子式 | C14H18F2N5Na4O12P3S |
分子量 | 703.26 |
溶解度 | <10mM in Water |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | The platelet P2T receptor plays a major role in platelet aggregation, and its antagonists are suggested to have significant therapeutic potential as antithrombotic agents. AR-C 66096 is a novel, potent and selective antagonist at human platelet P2T-purinoceptors. In vitro: In suspensions of human washed platelets, AR-C 66096 (1-100 nM) produced concentrationdependent rightward displacement of concentration-effect (E/[A]) curves obtained for ADP-induced platelet aggregation. The anti-aggregatory potency of AR-C 66096 was not influenced by increasing the incubation time from 2 to 15 min nor by inclusion of the P1-purinoceptor antagonist 8-sulphophenyltheophylline at a concentration (300 μM) [1]. In vivo: AR-C 66096 behaved as a weak (pA50 3.68) but full P2x-purinoceptor agonist in preparations of the isolated rabbit ear artery and as a weak, competitive antagonist (apparent pKB 4.71) at P2Y-purinoceptors in the isolated guinea-pig aorta, indicating a selectivity of at least 9000 fold for the Pzrsubtype. In the latter preparation, non-specific relaxations were observed by concentrations of AR-C 66096 >10 μM [1]. Clinical trial: Up to now, AR-C 66096 is still in the preclinical development stage. Reference: |