AR 244555

• CAT Number: I002680
• CAS Number: 858350-62-6
• Molecular Formula: C23H23ClF2N2O
• Molecular Weight: 416.89
• Purity: ≥95%
• IUPAC Name: (1'-but-3-enyl-5-chlorospiro[2H-indole-3,4'-piperidine]-1-yl)-(2,6-difluorophenyl)methanone
• InChI: InChI=1S/C23H23ClF2N2O/c1-2-3-11-27-12-9-23(10-13-27)15-28(20-8-7-16(24)14-17(20)23)22(29)21-18(25)5-4-6-19(21)26/h2,4-8,14H,1,3,9-13,15H2
• SMILES: C=CCCN1CCC2(CC1)CN(C3=C2C=C(C=C3)Cl)C(=O)C4=C(C=CC=C4F)F

Inverse agonist of Mas G-protein signaling (IC50 values 186 and 348 nM in human and rat inositol phosphatase (IP) Gq coupling assays respectively). AR 244555 caused a dose-dependent inhibition of inositol 1,4,5-trisphosphate accumulation in AdMas-infected cells, and attenuated the sarcomeric organization and cell enlargement observed in Mas overexpressing myocytes.AR 244555 caused a modest but significant increase in coronary flow in rat hearts witout causing arrhythmias, and provides protection from ischemia-reperfusion injury if administered either before ischemia or immediately before reperfusion.

Reference

T. Zhang et al. Inhibition of Mas G-protein signaling improves coronary blood flow, reduces myocardial infarct size, and provides long-term cardioprotection. Am. J. Physiol. Heart Circ. Physiol. 2012, 302, H299-311.