SML0981

RXFP1-Agonist-8

≥98% (HPLC)

• Synonym(s): 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide
• Empirical Formula (Hill Notation): C₂₄H₂₁F₃N₂O₅S
• CAS Number: 1482500-76-4
• Molecular Weight: 506.49
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

RXFP1-Agonist-8 is a potent selective agonist of the G-protein-coupled receptor RXFP1, human relaxin/insulin-like family peptide receptor 1, with an EC₅₀ of 94 nM in HEK293 cells and no activity with RXFP2 or RXFP3, other members of the relaxin family of receptors. RXFP1-Agonist-8 is believed to interact with an allosteric site at the ECL3 loop acting non-competitively with the natural hormone relaxin to activate RXFP1, and is the first bioavailable small-molecule agonist of human RXFP1 with good metabolic stability. Relaxin has long been known as a female hormone secreted by the corpus luteum that helps soften the cervix and relax the pelvic ligaments in childbirth. However, Relaxin also has potent cardiovascular and renal effects, inducing a 20% increase in cardiac output, 30% decrease in systemic vascular resistance, 30% increase in global arterial compliance and 45% increase in renal blood flow during pregnancy, anti-fibrotic, vasodilatory and pro-angiogenic effects that can be reproduced in both women and men with potential for treating various disorders including hypertensive diseases and acute heart failure.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable