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SR3335

Catalog No.
A3836
RORα agonist,partial inverse and selective
Grouped product items
SizePriceStock Qty
5mg
$85.00
In stock
10mg
$150.00
In stock
25mg
$300.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

SR3335 is a synthetic selective inverse agonist of RORα with Ki value of 220 nM [1][2].
The retinoic acid receptor-related orphan receptor α (RORα) is an orphan receptor that plays an important role in the regulation of metabolism.
SR3335 prevented the expression of endogenous RORα in HepG2. And it may suppress hepatic glucose production in type 2 diabetics. SR3335 was able to repress the expression of G6Pase. In ChIP trial, ML-176 reduced the amount of SRC2 at the G6Pase promoter [3]. In a GAL4-RORR ligand binding domain cotransfection assay, SR3335 inhibited the constitutive activity of RORα and the Ki was calculated as 220 nM [1].
When treat diet-induced obese mice with SR3335 (15 mg/kg), after injected with pyruvate, the plasma glucose levels were significantly lower at each time point compared with vehicle-treated animals. The results indicated SR3335 suppressed hepatic gluconeogenesis [1].
References:
[1]. Naresh Kumar, Douglas J. Kojetin, et al. Identification of SR3335 (ML176): a Synthetic RORα Selective Inverse Agonist. ACS Chem Biol. 2011 March 18; 6(3): 218-222.
[2]. Laura A. Solt, Thomas P. Burris. Action of RORs and their ligands in (patho)physiology. Trends in Endocrinology & Metabolism, 2012, 23(12): 619-627.
[3]. Kumar N, Nuhant P, Solt LA, et al. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Alpha (RORα). Probe Reports from the NIH Molecular Libraries Program [Internet], Bethesda (MD): National Center for Biotechnology Information (US),2010-.2010.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt405.34
Cas No.293753-05-6
FormulaC13H9F6NO3S2
SynonymsML-176;SR 3335;SR-3335;ML176;ML 176
Solubilityinsoluble in H2O; ≥87.4 mg/mL in EtOH; ≥88.8 mg/mL in DMSO
Chemical NameN-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]thiophene-2-sulfonamide
SDFDownload SDF
Canonical SMILESC1=CSC(=C1)S(=O)(=O)NC2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description SR3335 is a selective inverse agonist of retinoic acid receptor-related orphan receptor (ROR) RORα with IC50 value of 480 nM.
Targets RORα          
IC50 480 nM          

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