An allosteric agonist of RXFP1 (EC50 = 94 nM for human RXFP1); activates human

ML-290 – 10 mg

Brand:
Cayman
CAS:
1482500-76-4
Storage:
-20
UN-No:
Non-Hazardous - /

ML-290 is an allosteric agonist of relaxin family peptide receptor 1 (RXFP1; EC50 = 94 nM for human RXFP1).{33729,33731} It displays >15-fold selectivity for RXFP1 over RXFP2.{33731} ML-290 activates human, rhesus macaque, pig, and rabbit RXFP1 but is weak or inactive at mouse or guinea pig RXFP1.{33731,33730} Through RXFP1, ML-290 increases intracellular cAMP and induces VEGF expression (2.8-fold at 250 nM).{33731} ML-290 is metabolically stable and displays excellent in vivo pharmacokinetics.{33731}  

 

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Description

An allosteric agonist of RXFP1 (EC50 = 94 nM for human RXFP1); activates human, rhesus macaque, pig, and rabbit RXFP1 but is weak or inactive at mouse or guinea pig RXFP1; increases intracellular cAMP and induces VEGF expression

Formal name: 2-[[2-(1-methylethoxy)benzoyl]amino]-N-[3-[(trifluoromethyl)sulfonyl]phenyl]-benzamide

Synonyms:  RXFP1 Agonist 8​​

Molecular weight: 506.5

CAS: 1482500-76-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Neuroendocrinology

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