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CYM 50260

Names

[ CAS No. ]:
1355026-60-6

[ Name ]:
CYM 50260

Biological Activity

[Description]:

CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> LPL Receptor

[Target]

EC50: 45 nM (S1P4-R)[1]


[In Vitro]

CYM50260 (Compound 22aa) is a synthetic S1P4-R agonist. CYM50260 is found 3.5-fold more potent than the hit compound (HTS-hit)[1]. CYM50260 suppresses the collagen-stimulated platelet aggregation, PDGF-AB secretion and sCD40L release. CYM50260 reduces the release of phosphorylated-HSP27 by collagen as well as the phosphorylation of HSP27[2].

[References]

[1]. Guerrero M, et al. Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P₄-R) agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):537-42.

[2]. Onuma T, et al. Sphingosine 1-phosphate (S1P) suppresses the collagen-induced activation of human platelets via S1P4 receptor. Thromb Res. 2017 Aug;156:91-100.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H11Cl3FNO2

[ Molecular Weight ]:
350.60000

[ Exact Mass ]:
348.98400

[ PSA ]:
31.35000

[ LogP ]:
4.96910

Synthetic Route

Precursor & DownStream

Precursor

DownStream


Related Compounds

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