MRS 2279

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Cat.No. 2158 - MRS 2279 | C13H18ClN5O8P2.2NH3 | CAS No. 367909-40-8
Description: Selective, high affinity P2Y1 antagonist
Chemical Name: (1R*,2S*)-4-[2-Chloro-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester diammonium salt
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Literature

Biological Activity

Selective, high affinity competitive antagonist of the P2Y1 receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Fails to block nucleotide signaling at most other P2Y receptors (P2Y2, P2Y4, P2Y6, P2Y11 and P2Y12) and potently inhibits ADP-induced aggregation of human blood platelets in vitro (pKB = 8.05).

Licensing Information

Sold under license from the NIH, US Patent 10/169975

Technical Data

M. Wt 503.78
Formula C13H18ClN5O8P2.2NH3
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 367909-40-8
PubChem ID 90488744
InChI Key MLPKPDFUVMQAOX-KOVKCLEESA-N
Smiles ClC4=NC1=C(C(NC)=N4)N=CN1[C@H]2C[C@H](OP(O)(O)=O)[C@@]3(COP(O)(O)=O)[C@@H]2C3.N.N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 50.38 100

Preparing Stock Solutions

The following data is based on the product molecular weight 503.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.98 mL 9.92 mL 19.85 mL
5 mM 0.4 mL 1.98 mL 3.97 mL
10 mM 0.2 mL 0.99 mL 1.98 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Nandanan et al (2000) Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands. J.Med.Chem. 43 829 PMID: 10715151

Boyer et al (2002) 2-Chloro N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y1 receptor antagonist. Br.J.Pharmacol. 135 2004 PMID: 11959804

Kim et al (2003) 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J.Med.Chem 46 4974 PMID: 14584948


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Keywords: MRS 2279, supplier, Selective, high, affinity, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2279, Purinergic, P2Y, Receptors, Purinergic, P2Y, Receptors, Tocris Bioscience

3 Citations for MRS 2279

Citations are publications that use Tocris products. Selected citations for MRS 2279 include:

Ohtomo et al (2011) Increase of intracellular Ca2+ by purinergic receptors in cultured rat lacrimal gland myoepithelial cells. Invest Ophthalmol Vis Sci 52 9503 PMID: 22039237

Kuboyama et al (2011) Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia. Cell Death Dis 31 1930 PMID: 21487414

Harper and Poole (2010) Protein kinase Ctheta negatively regulates store-independent Ca2+ entry and phosphatidylserine exposure downstream of glycoprotein VI in platelets. J Biol Chem 285 19865 PMID: 20388711


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