1345858-76-5

1345858-76-5 structure

Name: CYM 50308
Chemical Name: (2Z,5Z)-5-{[1-(2,4-Difluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]me thylene}-2-[(2-methoxyethyl)imino]-3-methyl-1,3-thiazolidin-4-one
CAS Number: 1345858-76-5
Molecular Formula: C₂₀H₂₁F₂N₃O₂S
Molecular Weight: 405.461
Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
Create Date: 2016-04-10 16:22:07
Modify Date: 2024-01-02 18:26:55
CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM[1].

Name	(2Z,5Z)-5-{[1-(2,4-Difluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]me thylene}-2-[(2-methoxyethyl)imino]-3-methyl-1,3-thiazolidin-4-one
Synonyms	SIB 1553A hydrochloride 4-Thiazolidinone, 5-[[1-(2,4-difluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]methylene]-2-[(2-methoxyethyl)imino]-3-methyl-, (2Z,5Z)- (2Z,5Z)-5-{[1-(2,4-Difluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]methylene}-2-[(2-methoxyethyl)imino]-3-methyl-1,3-thiazolidin-4-one

Description	CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM[1].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> LPL Receptor
Target	EC50: 56 nM (S1P4-R), 2100 nM (S1P5-R)[1]
In Vitro	The disclosed lead molecule CYM50308 (Compound 24f) displays low nanomolar S1P4-R agonist activity and exquisite selectivity over the other S1P-Rs subtypes. Noteworthy, CYM50308 provides a valuable pharmacological tool to explore the effects of the S1P4-R signaling cascade and elucidate the molecular basis of the in vivo receptor function[1].
References	[1]. Urbano M, et al. Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6739-45.