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AR-C 66096 tetrasodium salt

Catalog No.
B5408
P2Y12 antagonist,potent and selective
Grouped product items
SizePriceStock Qty
1mg
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For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

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

Physical AppearanceColourless liquid
StorageStore at -20°C
M.Wt703.26
Cas No.145782-74-7
FormulaC14H18F2N5Na4O12P3S
Solubility<10mM in H2O
SDFDownload SDF
Canonical SMILESCCCSC1=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+]
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

AR-C 66096 tetrasodium salt