Cenerimod

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^[1][2]. In Vitro: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]. In Vivo: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].