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Chemical Compound Review

SureCN3810347     [(2R,3S,4R,5R)-3,4-dihydroxy- 5-[6-(2...

Synonyms: CTK2I5299, ARC69931MX, AR C69931MX, 847460-53-1
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Disease relevance of AR-C69931MX


High impact information on AR-C69931MX


Chemical compound and disease context of AR-C69931MX

  • CONCLUSIONS: As adjunctive therapy to aspirin and low-molecular-weight heparin in patients with unstable angina or non-Q-wave MI, intravenous AR-C69931MX was well tolerated, with no difference in the incidence of serious adverse events compared with placebo [2].

Biological context of AR-C69931MX


Anatomical context of AR-C69931MX


Associations of AR-C69931MX with other chemical compounds


Gene context of AR-C69931MX

  • On the contrary the effect on [Ca2+]i was neither inhibited by AR-C69931MX or by the P2Y1 antagonist MRS-2179 [6].
  • METHODS AND RESULTS: By using the selective P2 antagonists MRS2179 and AR-C69931MX, the P2Y12 receptor was found to be involved in thrombin-induced exposure of PS on isolated platelets and consequently in TF-induced thrombin formation in platelet-rich plasma [17].
  • AR-C69931MX (10 microM), a specific antagonist of the Gi-coupled P2Y12 ADP receptor, inhibits ERK2 activation induced by thrombin [13].
  • The actions of these agonists were significantly inhibited in the presence of the P2Y12 receptor antagonist, AR-C69931MX, but not the P2Y1 receptor antagonist, MRS2179 [18].
  • Clopidogrel (300 mg loading dose plus 75 mg daily) significantly inhibited TRAP-induced aggregation, procoagulant activity (annexin V binding) and microparticle production (all P < 0.05) but not as extensively as AR-C69931MX (400 nmol/l) [19].

Analytical, diagnostic and therapeutic context of AR-C69931MX


  1. Open multicentre study of the P2T receptor antagonist AR-C69931MX assessing safety, tolerability and activity in patients with acute coronary syndromes. Storey, R.F., Oldroyd, K.G., Wilcox, R.G. Thromb. Haemost. (2001) [Pubmed]
  2. Safety profile and tolerability of intravenous AR-C69931MX, a new antiplatelet drug, in unstable angina pectoris and non-Q-wave myocardial infarction. Jacobsson, F., Swahn, E., Wallentin, L., Ellborg, M. Clinical therapeutics. (2002) [Pubmed]
  3. Akt activation in platelets depends on Gi signaling pathways. Kim, S., Jin, J., Kunapuli, S.P. J. Biol. Chem. (2004) [Pubmed]
  4. A Gi-dependent pathway is required for activation of the small GTPase Rap1B in human platelets. Lova, P., Paganini, S., Sinigaglia, F., Balduini, C., Torti, M. J. Biol. Chem. (2002) [Pubmed]
  5. The nucleotide receptor P2Y13 is a key regulator of hepatic high-density lipoprotein (HDL) endocytosis. Jacquet, S., Malaval, C., Martinez, L.O., Sak, K., Rolland, C., Perez, C., Nauze, M., Champagne, E., Tercé, F., Gachet, C., Perret, B., Collet, X., Boeynaems, J.M., Barbaras, R. Cell. Mol. Life Sci. (2005) [Pubmed]
  6. Involvement of multiple P2Y receptors and signaling pathways in the action of adenine nucleotides diphosphates on human monocyte-derived dendritic cells. Marteau, F., Communi, D., Boeynaems, J.M., Suarez Gonzalez, N. J. Leukoc. Biol. (2004) [Pubmed]
  7. Inhibition of ADP-induced P-selectin expression and platelet-leukocyte conjugate formation by clopidogrel and the P2Y12 receptor antagonist AR-C69931MX but not aspirin. Storey, R.F., Judge, H.M., Wilcox, R.G., Heptinstall, S. Thromb. Haemost. (2002) [Pubmed]
  8. Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy. Ingall, A.H., Dixon, J., Bailey, A., Coombs, M.E., Cox, D., McInally, J.I., Hunt, S.F., Kindon, N.D., Teobald, B.J., Willis, P.A., Humphries, R.G., Leff, P., Clegg, J.A., Smith, J.A., Tomlinson, W. J. Med. Chem. (1999) [Pubmed]
  9. Synergistic action between inhibition of P2Y12/P2Y1 and P2Y12/thrombin in ADP- and thrombin-induced human platelet activation. Nylander, S., Mattsson, C., Ramström, S., Lindahl, T.L. Br. J. Pharmacol. (2004) [Pubmed]
  10. Prevention of arterial thrombosis by intravenously administered platelet P2T receptor antagonist AR-C69931MX in a canine model. Huang, J., Driscoll, E.M., Gonzales, M.L., Park, A.M., Lucchesi, B.R. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  11. Blockade of the platelet P2Y12 receptor by AR-C69931MX sustains coronary artery recanalization and improves the myocardial tissue perfusion in a canine thrombosis model. Wang, K., Zhou, X., Zhou, Z., Tarakji, K., Carneiro, M., Penn, M.S., Murray, D., Klein, A., Humphries, R.G., Turner, J., Thomas, J.D., Topol, E.J., Lincoff, A.M. Arterioscler. Thromb. Vasc. Biol. (2003) [Pubmed]
  12. Differential regulation of Rho and Rac through heterotrimeric G-proteins and cyclic nucleotides. Gratacap, M.P., Payrastre, B., Nieswandt, B., Offermanns, S. J. Biol. Chem. (2001) [Pubmed]
  13. ADP secretion and subsequent P2Y12 receptor signalling play a crucial role in thrombin-induced ERK2 activation in human platelets. Fälker, K., Lange, D., Presek, P. Thromb. Haemost. (2004) [Pubmed]
  14. Costimulation of the Gi-coupled ADP receptor and the Gq-coupled TXA2 receptor is required for ERK2 activation in collagen-induced platelet aggregation. Roger, S., Pawlowski, M., Habib, A., Jandrot-Perrus, M., Rosa, J.P., Bryckaert, M. FEBS Lett. (2004) [Pubmed]
  15. Platelet collagen receptor integrin alpha2beta1 activation involves differential participation of ADP-receptor subtypes P2Y1 and P2Y12 but not intracellular calcium change. Jung, S.M., Moroi, M. Eur. J. Biochem. (2001) [Pubmed]
  16. Effects on blood compatibility in vitro by combining a direct P2Y12 receptor inhibitor and heparin coating of stents. Christensen, K., Larsson, R., Emanuelsson, H., Elgue, G., Larsson, A. Platelets (2006) [Pubmed]
  17. Differential involvement of the P2Y1 and P2Y12 receptors in platelet procoagulant activity. Leon, C., Ravanat, C., Freund, M., Cazenave, J.P., Gachet, C. Arterioscler. Thromb. Vasc. Biol. (2003) [Pubmed]
  18. P2Y12 receptor-mediated potentiation of thrombin-induced thromboxane A2 generation in platelets occurs through regulation of Erk1/2 activation. Shankar, H., Garcia, A., Prabhakar, J., Kim, S., Kunapuli, S.P. J. Thromb. Haemost. (2006) [Pubmed]
  19. Inhibitory effects of P2Y12 receptor antagonists on TRAP-induced platelet aggregation, procoagulant activity, microparticle formation and intracellular calcium responses in patients with acute coronary syndromes. Behan, M.W., Fox, S.C., Heptinstall, S., Storey, R.F. Platelets (2005) [Pubmed]
  20. Preclinical and clinical studies with selective reversible direct P2Y12 antagonists. van Giezen, J.J., Humphries, R.G. Semin. Thromb. Hemost. (2005) [Pubmed]
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