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SML0981

Sigma-Aldrich

RXFP1-Agonist-8

≥98% (HPLC)

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

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

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SML0660SML1639SML2736
Sigma-Aldrich

Sigma-Aldrich

SML0981

RXFP1-Agonist-8

Sigma-Aldrich

Sigma-Aldrich

SML0660

GSK2578215A

BRD3308 ≥98% (HPLC)

Sigma-Aldrich

SML1639

BRD3308

NPBA ≥98% (HPLC)

Sigma-Aldrich

SML2736

NPBA

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to beige

color

white to beige

color

white to beige

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 15 mg/mL, clear

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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