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CYM 50308

Names

[ CAS No. ]:
1345858-76-5

[ Name ]:
CYM 50308

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
504.0±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C20H21F2N3O2S

[ Molecular Weight ]:
405.461

[ Flash Point ]:
258.6±32.9 °C

[ Exact Mass ]:
405.132263

[ PSA ]:
72.13000

[ LogP ]:
3.29

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.594

Related Compounds