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AR-C 66096 tetrasodium salt Sale

目录号 : GC12914

P2Y12 antagonist,potent and selective

AR-C 66096 tetrasodium salt Chemical Structure

Cas No.:145782-74-7

规格 价格 库存 购买数量
1mg
¥4,988.00
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Sample solution is provided at 25 µL, 10mM.

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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:
[1] Humphries, R.  G.; Tomlinson, W.; Ingall, A. H.; Cage, P. A.; Leff, P. FPL 66096: A Novel, Highly Potent and Selective Antagonist at Human Platelet P2T-purinoceptors. Br. J. Pharmacol. 1994, 113, 1057-1063.

Chemical Properties

Cas No. 145782-74-7 SDF
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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.4219 mL 7.1097 mL 14.2195 mL
5 mM 0.2844 mL 1.4219 mL 2.8439 mL
10 mM 0.1422 mL 0.711 mL 1.4219 mL
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