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
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.
Selective retinoic acid receptor-related receptor RORα partial inverse agonist that improves pyruvate tolerance in DIO mice in vivo.
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
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
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
The regulation of M1/M2 polarization in liver macrophages is closely associated with the progression of nonalcoholic steatohepatitis (NASH); however, the mechanism involved in this process remains unclear. Here, we describe the orphan nuclear receptor retinoic-acid-related orphan receptor α (RORα) as
Diabetic cardiomyopathy is a major complication that significantly contributes to morbidity and mortality in diabetics with few therapies. Moreover, antidiabetic drugs reported inconsistent or even adverse cardiovascular effects, suggesting that it is important to exploit novel therapeutic targets against diabetic
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