787548-03-2
Chemical Structure
Regrelor
Synonym(s): INS50589 free acid
- CAS No.: 787548-03-2
- Formula:C22H25N6O8P
- Molecular Weight:532.44
IUPAC Name: ((2S,3aR,4R,6R,6aR)-6-(6-(3-ethylureido)-9H-purin-9-yl)-2-((E)-styryl)tetrahydrofuro[3,4-d][1,3]dioxol-4-yl)methyl dihydrogen phosphate
InChIKey: NXHAXEBZOXCDKD-XIXRRVGJSA-N
SMILES: OP(OC[C@H]1O[C@@H](N(C=N2)C3=C2C(NC(NCC)=O)=NC=N3)[C@H]4[C@@H]1O[C@H](/C=C/C5=CC=CC=C5)O4)(O)=O
Biological Activity: Regrelor (INS50589 (free acid)) is a selective, reversible, and competitive P2Y12 receptor antagonist and an adenosine 5′-monophosphate derivative. Regrelor inhibits ADP (HY-W010918)-induced aggregation of human washed platelets with an IC50 of 0.016 μM. Intravenous infusion of Regrelor rapidly and dose-dependently inhibits ADP-induced platelet function, and platelet function gradually recovers after cessation of infusion. Regrelor can be used for research on P2Y12-mediated platelet function and cardiovascular regulation[1][2].
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Regrelor | Regrelor (INS50589 (free acid)) is a selective, reversible, and competitive P2Y12 receptor antagonist and an adenosine 5′-monophosphate derivative. Regrelor inhibits ADP (HY-W010918)-induced aggregation of human washed platelets with an IC50 of 0.016 μM. Intravenous infusion of Regrelor rapidly and dose-dependently inhibits ADP-induced platelet function, and platelet function gradually recovers after cessation of infusion. Regrelor can be used for research on P2Y12-mediated platelet function and cardiovascular regulation. | |||||||||||||||||||||
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References
- [1]. Douglass JG, et al. Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor. Journal of medicinal chemistry. 2008 Feb 28;51(4):1007-25. [Content Brief]
- [2]. Johnson FL, et al. Rapid and reversible modulation of platelet function in man by a novel P2Y(12) ADP-receptor antagonist, INS50589. Platelets. 2007 Aug;18(5):346-56.
