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。
| 生物活性 | SR12418 is aREV-ERB-specific synthetic ligandwithIC50s 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]. |
| IC50& Target | IC50: 68 nM (REV-ERBα) and 119 nM (REV-ERBβ)[1] |
体外研究
(In Vitro) | 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 andNfil3. |
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. |
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体内研究
(In Vivo) | 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 (CD44hi). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
