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CAS No.: 1335106-03-0

SR1001 Catalog No. CSN17703

SR1001 is a selective RORα and RORγ inverse agonist and inhibits TH17 cell differentiation and function.

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生物活性

实验方案

技术信息

生物活性

描述T helper cells that produce Interleukin-17 (IL-17) (T_H17 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 T_H17 cells. SR-1001 is an inverse agonist ligand of RORα/RORγ which dose dependently displaces [³H]25-hydroxycholesterol binding to RORα and RORγ (K_i = 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 T_S17 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].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT01776697 Healthy Phase 1 Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01776697	Healthy	Phase 1	Completed	-	-

[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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0947 mL
- 10.4734 mL
- 20.9467 mL
- 5 mM
- 0.4189 mL
- 2.0947 mL
- 4.1893 mL
- 10 mM
- 0.2095 mL
- 1.0473 mL
- 2.0947 mL

技术信息

CAS号

1335106-03-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H13F6N3O4S2

运输

蓝冰

分子量

477.40

别名

溶解度

DMSO	430.0 mg/mL (900.7 mM)
Water	insoluble

动物实验配方

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