AR-C 66096 tetrasodium salt


Catalog No. Size PriceQuantity
M22478-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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) . 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 . Clinical trial: Up to now, AR-C 66096 is still in the preclinical development stage.

Product information

CAS Number: 145782-74-7

Molecular Weight: 703.26

Formula: C14H18F2N5Na4O12P3S

Chemical Name: tetrasodium {[({[(2R,3S,4S,5R)-5-[6-amino-2-(propylsulfanyl)-9H-purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl phosphonato}oxy)(oxido)phosphoryl]difluoromethyl}phosphonate

Smiles: [Na+].[Na+].[Na+].[Na+].CCCSC1N=C2C(N=CN2[C@@H]2O[C@H](COP([O-])(=O)OP([O-])(=O)C(F)(F)P([O-])([O-])=O)[C@@H](O)[C@@H]2O)=C(N)N=1

InChiKey: IETVOLFQZIGNAQ-AKJNHRAGSA-J

InChi: InChI=1S/C14H22F2N5O12P3S.4Na/c1-2-3-37-13-19-10(17)7-11(20-13)21(5-18-7)12-9(23)8(22)6(32-12)4-31-36(29,30)33-35(27,28)14(15,16)34(24,25)26;;;;/h5-6,8-9,12,22-23H,2-4H2,1H3,(H,27,28)(H,29,30)(H2,17,19,20)(H2,24,25,26);;;;/q;4*+1/p-4/t6-,8-,9+,12-;;;;/m1..../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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