A P2Y1 receptor antagonist
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MRS2179 (ammonium salt hydrate)

Item No. 10011450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2′-deoxy-N-methyl-3′-adenylic acid, 5′-(dihydrogen phosphate), ammonium salt, hydrate
Molecular Formula
C11H17N5O9P2 • XNH3 [XH2O]
Formula Weight
425.2
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Water: 100 mM
SMILES
OP(OC[C@@H]1[C@@H](OP(O)(O)=O)C[C@H](N2C=NC3=C2N=CN=C3NC)O1)(O)=O.N.O
InChi Code
InChI=1S/C11H17N5O9P2.H3N.H2O/c1-12-10-9-11(14-4-13-10)16(5-15-9)8-2-6(25-27(20,21)22)7(24-8)3-23-26(17,18)19;;/h4-8H,2-3H2,1H3,(H,12,13,14)(H2,17,18,19)(H2,20,21,22);1H3;1H2/t6-,7+,8+;;/m0../s1
InChi Key
DEQIORFOBOEGKZ-ZJWYQBPBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $44

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    5 mg

    $142

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    10 mg

    $258

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    Product Description

    MRS2179 is a competitive purinergic P2Y1 receptor antagonist (Kb = 102 nM).1 It is selective for P2Y1 over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.2,3 MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate (2-MeSADP; Item No. 21230) with an IC50 value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1 receptor.1 It inhibits platelet shape change and aggregation induced by ADP (Item No. 21121) in washed isolated human platelets when used at a concentration of 10 µM.4 MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nandanan, E., Camaioni, E., Jang, S.-Y., et al. Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists. J. Med. Chem. 42(9), 1625-1638 (1999).

    2. von Kügelgen, I. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes. Pharmacol. Ther. 110(3), 415-432 (2006).

    3. Brown, S.G., King, B.F., Kim, Y.-C., et al. Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors. Drug Dev. Res. 49(4), 253-259 (2000).

    4. Tovar, C., Higgins, B., Deo, D.D., et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle 9(16), 3364-3375 (2010).

    5. Lenain, N., Freund, M., Léon, C., et al. Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist. J. Thromb. Haemost. 1(6), 1144-1149 (2003).