AZ7976 

AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC₅₀ > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research^[1].

AZ7976 (48h) has a cytotoxicity of IC₅₀=15 μM (THP1), 68/37 μM (HepG2 Glu/Gal), and 17 μM (HepG2 C3a spheroids). AZ7976's inhibitory effects on BSEP, hERG, NaV1.5, and KaV4.3 (Ikr) are IC₅₀=23 μM (BSEP), >39 μM (hERG), 231 μM (NaV1.5), and >33 μM (KaV4.3 (Ikr)), respectively. In the A549 micronucleus test, it shows negative genotoxicity^[1].
AZ7976 (90 min; concentration responses) does not compete with relaxin H2 for binding to RXFP1 in CHO-hRXFP1 cells, but enhances 125I-relaxin H2 binding^[1].
AZ7976 inhibits ion channels and bile salt efflux transporter (BSEP) and is cytotoxic to THP1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZ7976 (i.v.; initial 1.5 mg/kg; i.v.drip; continuous 9.0 mg/kg) causes a significant increase in heart rate and a rise in mean arterial blood pressure in the rats.^[1].

Pharmacokinetic Analysis in AZ7976^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

682.65

C₃₀H₃₃F₇N₂O₆S

2813866-27-0

COC1=CC(F)=C(C=C1C(N[C@H]2[C@H]([C@@H]3CC[C@H]2C3)C(NC4=CC=C(C(S(F)(F)(F)(F)F)=C4)F)=O)=O)O[C@H]5CC[C@](C)(CC5)C(O)=O

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• [1]. Granberg KL, et al. Identification of Novel Series of Potent and Selective Relaxin Family Peptide Receptor 1 (RXFP1) Agonists. J Med Chem. 2024 Mar 28;67(6):4442-4462.   [Content Brief]