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Merck
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Key Documents

SML0981

Sigma-Aldrich

RXFP1-Agonist-8

≥98% (HPLC)

别名:

2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide

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About This Item

经验公式(希尔记法):
C24H21F3N2O5S
分子量:
506.49
分類程式碼代碼:
51111800
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 10 mg/mL, clear

儲存溫度

2-8°C

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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