| 產(chǎn)品描述： | SR1001是RORα的反向激動(dòng)劑，對(duì)RORα和RORγ的Ki值分別為172 nM和111 Nm |
| 靶點(diǎn)： |
RORγ:111 nM(Ki); RORα:172 nM(Ki);ROR |
| 體外研究： |
SR1001 binds specifically to the ligand binding domains (LBDs) of RORα and RORγt inducing a conformational change within the LBD that encompasses repositioning of helix 12 leading to diminished affinity for coactivators and increased affinity for corepressors resulting in suppression of the receptors transcriptional activity |
| 體內(nèi)研究： |
SR1001 suppresses the immune response, including TH17 cells in vitro and in vivo, TH1 cells in vivo, autoantibody production, maintains insulin levels, and increases Foxp3 expression. SR1001 effectively protects against pathologic neovascularization in both oxygen-induced retinopathy and another angiogenic model of very-low-density lipoprotein receptor (Vldlr)-deficient (Vldlr ?/?) mice with spontaneous subretinal neovascularization |
| 動(dòng)物實(shí)驗(yàn)： |
Animal Models: Female NOD/LtJ mice Dosages: 25 mg/kg Administration: IP |
| 參考文獻(xiàn)： |
1. Laura A. Solt, et al. ROR Inverse Agonist Suppresses Insulitis and Prevents Hyperglycemia in a Mouse Model of Type 1 Diabetes. Endocrinology. 2015, 156(3): 869-881. 2. Laura A. Solt, et al. Suppression of TH17 Differentiation and Autoimmunity by a Synthetic ROR Ligand. Nature. 2011, 472(7344): 491-494. 3. Sun Y, et al. Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation. Proc Natl Acad Sci U S A. 2015, 112(33):10401-6. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.095 ml |
10.473 ml |
20.947 ml |
| 5 mM |
0.419 ml |
2.095 ml |
4.189 ml |
| 10 mM |
0.209 ml |
1.047 ml |
2.095 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.419 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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