CS 2100

Names

[ Name ]:
CS 2100

[Synonym ]:
1-({4-[1-(3-oxo-3-phenyl-propyl)-1H-benzoimidazol-2-ylmethyl]-piperazin-1-yl}-acetyl)-pyrrolidine
1-({4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl}methyl)azetidine-3-carboxylic acid
Pyrrolidine,1-((4-((1-(3-oxo-3-phenylpropyl)-1H-benzimidazol-2-yl)methyl)-1-piperazinyl)acetyl)
1-(2'-Benzoyleth-1'-yl)-2-(4''-pyrrolidinocarbonylmethylpiperazine-1''-ylmethyl)benzimidazole

Biological Activity

[Description]:

CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

Research Areas >> Inflammation/Immunology

[Target]

EC50: 4.0 nM (human S1P1)[1]

[References]

[1]. Nakamura T, et al. Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1788-92.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₃N₃O₄S

[ Molecular Weight ]:
461.53

[ Exact Mass ]:
461.14100

[ PSA ]:
116.93000

[ LogP ]:
5.27410

Synthetic Route

Click to get detail synthetic route

Related Compounds

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