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SR1001 ROR agonist

Name: SR1001
Brand: Selleck Chemicals
SKU: S6724
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6724

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

Chemical Structure

Molecular Weight: 477.40

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Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Other ROR Inhibitors	SR1078 GSK2981278 TMP778 Cintirorgon (LYC-55716) S18-000003 Cedirogant Neoruscogenin SR3335

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (198.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.75mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.68mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	477.40	Formula	C₁₅H₁₃F₆N₃O₄S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1335106-03-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	RORγ 111 nM(Ki) RORα 172 nM(Ki)
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.
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. This compound 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.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4330305/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3148894/ [3] https://pubmed.ncbi.nlm.nih.gov/26243880/

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Handling Instructions

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