1. Metabolic Enzyme/Protease
  2. ROR
  3. SR1001

SR1001 

Cat. No.: HY-13421 Purity: 99.79%
Handling Instructions

SR1001 is a selective RORα and RORγ inverse agonist with Kis 172 and 111 nM, respectively.

For research use only. We do not sell to patients.

SR1001 Chemical Structure

SR1001 Chemical Structure

CAS No. : 1335106-03-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 744 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

SR1001 is a selective RORα and RORγ inverse agonist with Kis 172 and 111 nM, respectively.

In Vitro

SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells[1].

In Vivo

SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1[1]. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 39 mg/mL (81.69 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0947 mL 10.4734 mL 20.9468 mL
5 mM 0.4189 mL 2.0947 mL 4.1894 mL
10 mM 0.2095 mL 1.0473 mL 2.0947 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

HEK293 cells are plated in 96-well plates at a density of 15 x 103 cells/well. Transfections are performed using Lipofectamine 2000. 24 h post-transfection, the cells are treated with vehicle or compound (SR1001). 24 h post-treatment, the luciferase activity is measured using the Dual-Glo luciferase assay system[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Experimental autoimmune encephalomyelitis is induced in C57BL/6 wild-type mice by s.c. injection over four sites in the flank with 200 μg per mouse. The SR1001 is dissolved in DMSO at 25 mg/mL and the mice are treated (i.p.) with 25 mg/kg SR1001 (1 μL/g body weight of mouse) or vehicle (DMSO, 1 μL/g body weight of mouse) twice per day. The treatment is started 2 days before immunization and continued until the end of experiment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

477.40

Formula

C₁₅H₁₃F₆N₃O₄S₂

CAS No.

1335106-03-0

SMILES

CC(NC1=NC(C)=C(S(=O)(NC2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O)S1)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SR1001
Cat. No.:
HY-13421
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SR1001

Cat. No.: HY-13421