Home Transmembrane Transporters ROR agonist SR1001 For research use only.

SR1001

SR1001 is a RORα inverse agonist with Ki values of 172 nM and 111 nM for RORα and RORγ respectively.

SR1001 Chemical Structure

SR1001 Chemical Structure

CAS No. 1335106-03-0

Purity & Quality Control

SR1001 Related Products

Biological Activity

Description SR1001 is a RORα inverse agonist with Ki values of 172 nM and 111 nM for RORα and RORγ respectively.
Targets
RORγ [2] RORα [2]
111 nM(Ki) 172 nM(Ki)
In vitro
In vitro

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[2].
In Vivo
In vivo

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[1]. 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[3].
Animal Research Animal Models Female NOD/LtJ mice
Dosages 25 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 477.40 Formula

C15H13F6N3O4S2
CAS No. 1335106-03-0 SDF --
Smiles CC1=C(SC(=N1)NC(=O)C)S(=O)(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (198.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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