RXFP1-Agonist-8
SIGMA/SML0981 - ≥98% (HPLC)
Synonym: 2-
CAS Number: 1482500-76-4
Empirical Formula (Hill Notation): C24H21F3N2O5S
Molecular Weight: 506.49
Linear Formula: C24H21F3N2O5S
Product Type: Chemical
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| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| Quality Level | 100  |
| solubility | DMSO: 10 mg/mL, clear |
| storage temp. | 2-8°C |
| 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, |
| 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. |
| Packaging: | 5, 25 mg in glass bottle |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 51111800 |