Cenerimod

Research use only, not for human use.

Cenerimod (ACT-334441) is a potent and orally available S1P1 receptor agonist with EC50 of 2.7 nM.

Cenerimod (ACT-334441) is a potent and orally available S1P1 receptor agonist with EC50 of 2.7 nM; shows a powerful and long-lasting immunomodulating effect by reducing the number of circulating and infiltrating T- and B-lymphocytes, without affecting their maturation, memory, or expansion.Multiple Sclerosis Phase 1 Clinical.

Cenerimod is a highly potent S1P1 receptor agonists in (35S)-GTPγS assays using HUVEC cell membrane preparations, with an EC50 of 2 nM.Cenerimod activates G protein and increases Ca2+ signaling in CHO cells, with EC50s of 1 nM and 124 nM, respectively.Cenerimod (5 μM; 24 h) inhibits collagen production in fibroblasts.

Cenerimod (0.1-10 mg/kg; a single p.o.) reversibly reduces the number of circulating lymphocytes in a dose-dependent manner in rats.Cenerimod (6 mg/kg/day for 30 days; p.o.) attenuates disease in a mouse experimental autoimmune encephalitis (EAE) model.Cenerimod (10 mg/kg/day for 42 days; p.o.) attenuates skin and lung fibrosis in Scl-cGVHD mice. Animal Model:Male Wistar rats weighing 294-510 g Dosage:0.1, 0.3, 1, 3 and 10 mg/kg Administration:A single p.o.Result:Effectively and reversibly reduced the blood lymphocyte counts, with a plateau reached after a single oral dose of 1 mg/kg.

ACT-334441

GPCR/G Protein

Lysophospholipid Receptor

Lysophospholipid Receptor

Inflammation/Immunology

Multiple Sclerosis

1262414-04-9

453.5307

C25H31N3O5

>98% (HPLC)

10 mM in DMSO

OC[C@H](O)COC1=C(C)C=C(C2=NOC(C3=CC(C4CCCC4)=NC(OC)=C3)=N2)C=C1CC

1,2-Propanediol, 3-[4-[5-(2-cyclopentyl-6-methoxy-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]-, (2S)-

(-20℃)

With Ice Pack

≥ 2 years