A selective inverse agonist of RORα

SR 3335 – 1 mg

Brand:
Cayman
CAS:
293753-05-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}  

 

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SKU: 12072 - 1 mg Category:

Description

A selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM); evokes RORα-dependent effects both in vitro and in vivo

Formal name: N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-2-thiophenesulfonamide

Synonyms:  ML 176

Molecular weight: 405.3

CAS: 293753-05-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs

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