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SR 3335 (CAS 293753-05-6) LS-H85

ROR alpha agonist
LS-H85-1 / 1 mg / $175
LS-H85-5 / 5 mg / $225
LS-H85-10 / 10 mg / $265
LS-H85-25 / 25 mg / $395
USA Shipment Only
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Description: The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles. SR 3335 is a selective inverse agonist of ROR alpha, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM). It is without effect on ROR beta, ROR gamma, farnesoid X receptor, or liver X receptor alpha . SR 3335 evokes ROR alpha -dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis. H85_ChemicalStructureImage.png
N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-2-thiophenesulfonamide
ML176
biochemical, chemical, agonist
LS-H85
293753-05-6
C13H9F6NO3S2
≥95%
A crystalline solid
 
OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(NS(C2=CC=CS2)(=O)=O)C=C1
InChI=1S/C13H9F6NO3S2/c14-12(15,16)11(21,13(17,18)19)8-3-5-9(6-4-8)20-25(22,23)10-2-1-7-24-10/h1-7,20-21H
LZWUNZRMANFRAO-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: RORA / ROR Alpha related products

Usage Information

SR 3335 is supplied as a crystalline solid. A stock solution may be made by dissolving the SR 3335 in the solvent of choice. SR 3335 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of SR 3335 in these solvents is approximately 33, 16, and 20 mg/ml, respectively. SR 3335 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, SR 3335 should first be dissolved in ethanol and then diluted with the aqueous buffer of choice. SR 3335 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of ethanol:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nat. Lett. 472(7344), 491-4 (2011).
  2. Jetten, A.M. and Ueda, E. Retinoid-related orphan receptors (RORs): Roles in cell survival, differentiation and disease. Cell Death and Different 9(11), 1167-1171 (2002).
  3. Ivanov, I.I., McKenzie, B.S., Zhou, L., et al. The orphan nuclear receptor RORγt directs the differentiation program of proinflammatory IL-17+ T helper cells. Cell 126, 1121-1133 (2006).
  4. Kumar, N., Kojetin, D.J., Solt, L.A., et al. Identification of SR3335 (ML176): A synthetic RORα selective inverse agonist. ACS Chem. Biol. 6(3), 218-222 (2011).

 


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