854107-55-4

854107-55-4 structure

Name: Ponesimod
Chemical Name: (5Z)-5-[[3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl]methylidene]-3-(2-methylphenyl)-2-propylimino-1,3-thiazolidin-4-one
CAS Number: 854107-55-4
Molecular Formula: C₂₃H₂₅ClN₂O₄S
Molecular Weight: 460.974
Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
Create Date: 2017-04-26 12:25:59
Modify Date: 2024-01-02 10:00:28
Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.IC50 value: Target: S1P1 agonistin vitro: Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC(50) of 5.7 nM) and selectivity [1]. in vivo: Oral administration of ponesimod to rats led to a dose-dependent decrease of blood lymphocyte count. After discontinuation of dosing, blood lymphocyte count returned to baseline within 48 h. Ponesimod prevented edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity [1].

Name	(5Z)-5-[[3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl]methylidene]-3-(2-methylphenyl)-2-propylimino-1,3-thiazolidin-4-one
Synonyms	UNII-5G7AKV2MKP Ponesimod (2Z,5Z)-5-{3-Chloro-4-[(2R)-2,3-dihydroxypropoxy]benzylidene}-3-(2-methylphenyl)-2-(propylimino)-1,3-thiazolidin-4-one 4-Thiazolidinone, 5-[[3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl]methylene]-3-(2-methylphenyl)-2-(propylimino)-, (2Z,5Z)- ACT-128800

Description	Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.IC50 value: Target: S1P1 agonistin vitro: Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC(50) of 5.7 nM) and selectivity [1]. in vivo: Oral administration of ponesimod to rats led to a dose-dependent decrease of blood lymphocyte count. After discontinuation of dosing, blood lymphocyte count returned to baseline within 48 h. Ponesimod prevented edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity [1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> LPL Receptor Research Areas >> Inflammation/Immunology
References	[1]. Piali L, et al. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011 May;337(2):547-56. [2]. Bolli MH, et al. 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010 May 27;53(10):4198-211. [3]. Brossard P, et al. Pharmacokinetics and pharmacodynamics of ponesimod, a selective S1P1 receptor modulator, in the first-in-human study. Br J Clin Pharmacol. 2013 Dec;76(6):888-96.