SR12418 是一种REV-ERB特异性合成配体，对 REV-ERBα 和 REV-ERBβ 的IC50值分别为 68 nM 和 119 nM。SR12418 可用于实验性自身免疫性脑脊髓炎 (EAE) 和结肠炎的研究。

SR12418 is a REV-ERB-specific synthetic ligand with IC 50 s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research [1] [2].

SR12418 (5 μM; 96 h) inhibits the growth of TH17 cells [1]. SR12418 (5 and 10 μM; 4 d) inhibits cell differentiation under TH17 polarizing conditions [1]. RT-PCR [1] Cell Line: TH17 cells Concentration: 5 μM Incubation Time: 96 hours Result: Repressed TH17-mediated gene expression and Nfil3. Cell Differentiation Assay [1] Cell Line: Mouse CD4 + T cells Concentration: 5 and 10 μM Incubation Time: 4 days Result: Inhibited TH17 cell differentiation in a dose-dependent manner.

SR12418 (intraperitoneal injection; 50 mg/kg; twice a day) suppresses the development and severity of experimental autoimmune encephalomyelitis [1]. SR12418 (intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization) shows effects in intervention studies of relapsing-remitting experimental autoimmune encephalomyelitis [1]. Animal Model: C57BL/6 mice inducing experimental autoimmune encephalomyelitis (EAE) [1] Dosage: 50 mg/kg Administration: Intraperitoneal injection; 50 mg/kg; twice a day Result: Diminished the incidence of disease with approximately 20% mice developing disease. Showed no overt signs of toxicity. Animal Model: PLP139-151-induced relapsing-remitting EAE (R-EAE) in SJL/J mice [1] Dosage: 50 mg/kg Administration: Intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization Result: Resulted in a significant reduction in the relapse severity compared to the vehicle control. Showed a significant decrease in the frequency and number of CD4 + and CD8 + effector cells (CD44 hi ).

1801185-08-9

C31H30FNO3

483.57

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years