GLPBio

SR 1001

Catalog No.: GC15009Purity:>99.50%
COASDSData Sheet
RORα and γ inverse agonist

Products are for research use only. Not for human use. We do not sell to patients.

SR 1001
Cas No.: 1335106-03-0
10mM (in 1mL DMSO)In Stock
$56.00
1
1mgIn Stock
$21.00
1
5mgIn Stock
$53.00
1
10mgIn Stock
$87.00
1
25mgIn Stock
$203.00
1
50mgIn Stock
$326.00
1
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Description

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

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].

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].

References:
[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]. 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.

Protocol

Cell experiment:

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].

Animal experiment:

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].

References:

[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]. 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1335106-03-0
Chemical Name
(Z)-N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)sulfamoyl)-4-methylthiazol-2-yl)acetimidic acid
SMILES
CC1=C(S(NC2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)(=O)=O)SC(/N=C(O)/C)=N1
Molecular Formula
C15H13F6N3O4S2
Molecular Weight
477.4
Solubility
≥ 102.4 mg/mL in DMSO, ≥ 17.1 mg/mL in EtOH
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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