B7-33 is a single-chain relaxin mimetic and a selective relaxin receptor 1 ( RXFP1 ) agonist. B7-33 phosphorylates ERK1/2 without inducing activation of the cAMP signaling pathway. B7-33 exhibits anti-fibrotic and cardioprotective activities. B7-33 can be used in the research of vascular diseases such as cardiomyopathy, myocardial infarction and fibrosis [1] [2].
In Vivo, B7-33 (0.25 mg/kg; i.p.; twice daily; 7 days) exerts a protective effect in a mouse model of ischemia-reperfusion[1]. B7-33 (0.25 mg/kg; s.c.; 7 days) exerts cardioprotective effects in a mouse model of cardiomyopathy[2].
In Vitro, B7-33 (10-100 nM) increases the survival rate of primary adult mouse cardiomyocytes subjected to simulated ischemia-reperfusion treatment via an ERK 1/2-dependent mechanism[1]. B7-33 (10-100 nM; 12 h) increases the survival rate of primary adult mouse cardiac fibroblasts subjected to simulated ischemia-reperfusion[1]. B7-33 (10-100 nM) dose-dependently increases the phosphorylation level of ERK1/2 in primary cardiomyocytes of adult mice[1]. B7-33 (100 nM; 24 h) reduces the expression of inflammasome marker ASC and endoplasmic reticulum stress marker GRP78 in adult primary mouse cardiomyocytes subjected to simulated ischemia-reperfusion[1].
References:
[1]. Devarakonda T, et al. B7-33, a Functionally Selective Relaxin Receptor 1 Agonist, Attenuates Myocardial Infarction-Related Adverse Cardiac Remodeling in Mice. J Am Heart Assoc. 2020;9(8):e015748.
[2]. Alam F, et al. The single-chain relaxin mimetic, B7-33, maintains the cardioprotective effects of relaxin and more rapidly reduces left ventricular fibrosis compared to perindopril in an experimental model of cardiomyopathy. Biomed Pharmacother. 2023;160:114370.
In Vivo, B7-33 (0.25 mg/kg; i.p.; twice daily; 7 days) exerts a protective effect in a mouse model of ischemia-reperfusion[1]. B7-33 (0.25 mg/kg; s.c.; 7 days) exerts cardioprotective effects in a mouse model of cardiomyopathy[2].
In Vitro, B7-33 (10-100 nM) increases the survival rate of primary adult mouse cardiomyocytes subjected to simulated ischemia-reperfusion treatment via an ERK 1/2-dependent mechanism[1]. B7-33 (10-100 nM; 12 h) increases the survival rate of primary adult mouse cardiac fibroblasts subjected to simulated ischemia-reperfusion[1]. B7-33 (10-100 nM) dose-dependently increases the phosphorylation level of ERK1/2 in primary cardiomyocytes of adult mice[1]. B7-33 (100 nM; 24 h) reduces the expression of inflammasome marker ASC and endoplasmic reticulum stress marker GRP78 in adult primary mouse cardiomyocytes subjected to simulated ischemia-reperfusion[1].
References:
[1]. Devarakonda T, et al. B7-33, a Functionally Selective Relaxin Receptor 1 Agonist, Attenuates Myocardial Infarction-Related Adverse Cardiac Remodeling in Mice. J Am Heart Assoc. 2020;9(8):e015748.
[2]. Alam F, et al. The single-chain relaxin mimetic, B7-33, maintains the cardioprotective effects of relaxin and more rapidly reduces left ventricular fibrosis compared to perindopril in an experimental model of cardiomyopathy. Biomed Pharmacother. 2023;160:114370.