ML 176, ML-176, ML176, N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)thiophene-2-sulfonamide, N-[4-[2,2,2-Trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-2-thiophenesulfonamide, SR 3335, SR-3335
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SR3335 is a selective partial inverse agonist against the retinoic acid receptor-related orphan receptor ROR-alpha (RORα LBD Ki = 220 nM) that selectively inhibits the constitutive transactivation activity of RORα (IC50 = 480 nM), but not RORβ, RORγ or LXRα, by cell-based reporter assays without affinity toward other RORs. SR3335 effectively suppresses HepG2 cellular RORα target genes expression (5 μM) and improves pyruvate tolerance in DIO mice in vivo (15 mg/kg bid. Ip.) by suppressing gluconeogenesis.
Several nuclear receptors (NRs) are still character-ized as orphan receptors because ligands have not yet been identified for these proteins. The retinoic acid receptor-related receptors (RORs) have no well-defined physiological ligands. Here, we describe the identification of a selective RORα
American journal of physiology. Lung cellular and molecular physiology, 312(6), L983-L993 (2017-04-01)
Early-life wheezing-associated respiratory tract infection by rhinovirus (RV) is considered a risk factor for asthma development. We have shown that RV infection of 6-day-old BALB/c mice, but not mature mice, induces an asthmalike phenotype that is associated with an increase
The Journal of investigative dermatology, 137(12), 2523-2531 (2017-08-05)
The retinoic acid receptor-related orphan receptors RORα and RORγ are critical for the functions of specific subsets of T cells and innate lymphoid cells, which are key drivers of inflammatory disease in barrier tissues. Here, we investigate the anti-inflammatory potential
The RORα-deficient staggerer (sg/sg) mouse is lean and resistant to diet-induced obesity. Its thermogenic activity was shown to be increased not only in brown adipose tissue (BAT), but also in subcutaneous white adipose tissue (WAT) where UCP1 content was enhanced
Journal of leukocyte biology, 102(6), 1451-1460 (2017-09-28)
Gut microbiota that invades to the defective mucosal barrier is one of the major sources of infectious complications in severely burned hosts. In this study, a role of group 2 innate lymphoid cells (ILC2) and effects of N-{4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}-2-thiophenesulfonamide (SR3335) on
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