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Metabolism ROR SR1001

SR1001

Catalog No. T5163   CAS 1335106-03-0
Purity 99.04% Datasheet

SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).

SR1001, CAS 1335106-03-0
Pack Size Availability Price/USD Quantity
5 mg In stock 89.00
10 mg In stock 155.00
50 mg In stock 720.00
100 mg In stock 1080.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).
Targets&IC50 RORα :ic50 172 nM (Ki),   RORγ :ic50 111 nM (Ki),  
Cell Research
CD4+ T cells were isolated as described previously and in the Supplementary Materials. CD4+ T cells cultured with splenic feeder cells were activated with 2.5 ?g/mL of anti-CD3 (clone 145–11), and differentiated to Th17 cells by addition of IL-6 (20 ng/mL; Peprotech), TGFβ (5 ng/mL), anti-IL-4 (10 ?g/mL; clone 11B11, UAB core facility) and anti-IFNγ (10 ?g/mL; clone XMG1.2, UAB core facility). After 5 days of differentiation toward Th17 cells, cells were recovered after histopaque gradient purification and resuspended in PBS. An aliquot of cells was used to evaluate the percent of Th17 cells (~40%) and ~10–20×106 undifferentiated CD4+ T or Th17 cells were injected in 500 ?L PBS by tail vein 48 h prior to behavioral testing. Where indicated, mice were injected intraperitoneally with 100 ?g anti-IL-17A, or 125 ?g SR1001 daily beginning 1 day before Th17 cell transfer, and this was continued throughout the experiment. As controls, mice were injected i.v. with ~10–20×106 CD4+ T cells to evaluate the effect of non-differentiated cells, or with 500 ?L PBS to mimic the stress of tail vein i.v. injection 48 h prior to behavioral testing. Intracellular cytokine staining was carried out as described previously and in the Supplementary Information [2].
Animal Research
For circadian gene expression experiments male C57BL6 mice (8–10 weeks of age) were either maintained on a L:D (12h∶12h) cycle or on constant darkness (1 day). At the circadian time (CT) 0 animals were administered a single dose of 25 mg/kg SR1001 (i.p.) and groups of animals (n?=?6) were sacrificed at CT0, CT6, CT12, and CT18. Gene expression was determined by real-time qPCR. Gene expression was normalized to Cyclophin b in all experiments [3].
Molecular Weight 477.4
Formula C15H13F6N3O4S2
CAS No. 1335106-03-0

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 45 mg/mL

Ethanol: 45 mg/mL

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. 2. Beurel E, et al. Inflammatory T helper 17 cells promote depression-like behavior in mice. Biol Psychiatry. 2013 Apr 1;73(7):622-30. 3. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804.

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