产品说明书
SR1001
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同义名 : | - |
| CAS号 : | 1335106-03-0 | |
| 货号 : | A240693 | |
| 分子式 : | C15H13F6N3O4S2 | |
| 纯度 : | 98% | |
| 分子量 : | 477.402 | |
| MDL号 : | MFCD23160036 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 40 mg/mL(83.79 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | T helper cells that produce Interleukin-17 (IL-17) (TH17 cells) are a recently identified CD4+ T-cell subset with characterized pathological roles in autoimmune diseases. The nuclear receptors retinoic-acid-receptor-related orphan receptors α and γt (RORα and RORγt, respectively) are required for the full differentiation of naïve CD4+ T cells into TH17 cells. SR-1001 is an inverse agonist ligand of RORα/RORγ which dose dependently displaces [3H]25-hydroxycholesterol binding to RORα and RORγ (Ki = 172 and 111 nM, respectively). In HEK293 cells, SR-1001 repressed both GAL4-RORα and GAL4-RORγ transcriptional activity in a dose dependent manner. Also in HEK293 cells transfected with the Il17 reporter and either full-length RORα or RORγ, SR-1001 dose-dependently suppressed the Il17 promoter driven activity by each of the receptors. In EL4 cells expressing RORα, RORγt and IL-17A (Il17α), treatment of cells with SR-1001 suppressed Il17α mRNA expression indicating that SR-1001 suppression of Il17α mRNA expression is RORα/RORγ dependent. In an animal model of TS17 cell-mediated autoimmune disease, 25 mg/kg of SR-1001 b.i.d. i.p. delayed the onset and clinical severity of EAE (experimental autoimmune encephalomyelitis)[3]. | ||
| 作用机制 | SR-1001 binds specifically to the ligand binding domains (LBDs) of RORα and RORγt inducing a conformational change within the LBD[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.47mL 2.09mL 1.05mL |
20.95mL 4.19mL 2.09mL |
| 参考文献 |
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