CenerimodCenerimod
MedChemExpress (MCE)
HY-17606
1262414-04-9
ACT-334441
99.43%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
Cenerimod is a highly potent S1P1 receptor agonists in (35S)-GTPγS assays using HUVEC cell membrane preparations, with an EC50 of 2 nM[1]. Cenerimod activates G protein and increases Ca2+ signaling in CHO cells, with EC50s of 1 nM and 124 nM, respectively[1]. Cenerimod (5 μM
24 h) inhibits collagen production in fibroblasts[2].
Cenerimod (0.1-10 mg/kg
a single p.o.) reversibly reduces the number of circulating lymphocytes in a dose-dependent manner in rats[1]. Cenerimod (6 mg/kg/day for 30 days
p.o.) attenuates disease in a mouse experimental autoimmune encephalitis (EAE) model[1]. Cenerimod (10 mg/kg/day for 42 days
p.o.) attenuates skin and lung fibrosis in Scl-cGVHD mice[2].
S1PR1 1 nM (EC50) S1PR5 36 nM (EC50) S1PR5 228 nM (EC50) S1PR4 2134 nM (EC50)
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[1]. Piali L, et, al. Cenerimod, a novel selective S1P 1 receptor modulator with unique signaling properties. Pharmacol Res Perspect. 2017 Dec
5(6):e00370. [Content Brief]
[2]. Kano M, et, al. Attenuation of murine sclerodermatous models by the selective S1P 1 receptor modulator cenerimod. Sci Rep. 2019 Jan 24
9(1):658. [Content Brief]