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SR1001 {[allProObj[0].p_purity_real_show]}

货号:A240693

SR1001是一种选择性的 RORα 和 RORγ 反向激动剂,能抑制 TH17 细胞分化和功能。

SR1001 化学结构 CAS号:1335106-03-0
SR1001 化学结构
CAS号:1335106-03-0
SR1001 3D分子结构
CAS号:1335106-03-0
SR1001 化学结构 CAS号:1335106-03-0
SR1001 3D分子结构 CAS号:1335106-03-0
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SR1001 纯度/质量文件 产品仅供科研

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SR1001 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].

SR1001 参考文献

[1]Crumbley C, Wang Y, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804.

[2]Solt LA, Kumar N, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4.

[3]Solt LA, Kumar N, Nuhant P, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011;472(7344):491-494

SR1001 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.95mL

4.19mL

2.09mL

SR1001 技术信息

CAS号1335106-03-0
分子式C15H13F6N3O4S2
分子量 477.402
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

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

动物实验配方
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