AZ7976_product_DataBase

Bioactivity	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].
Invitro	AZ7976 (90 min; concentration responses) 在 CHO-hRXFP1 细胞中不与 relaxin H2 竞争结合 RXFP1，而是增强了 125I-relaxin H2 的结合[1]。AZ7976 抑制离子通道和 bile salt efflux transporter (BSEP)，对 THP1 具有细胞毒性[1]。In Vitro Safety[1]
In Vivo	AZ7976 (i.v.; 初次给药 1.5 mg/kg; i.v.drip; 持续给药 9.0 mg/kg) 导致大鼠心率显著增加，平均动脉血压升高[1]。药代动力学分析[1] Route
CAS	2813866-27-0
Formula	C30H33F7N2O6S
Molar Mass	682.65
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB