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GSK2981278
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2981278图片
CAS NO:1474110-21-8
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 461.61
FormulaC25H35NO5S
CAS No.1474110-21-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES O=S(C1=CC=C(OCC2CCOCC2)C(CO)=C1)(N(C3=CC=C(CC)C=C3)CC(C)C)=O
Synonyms GSK-2981278; GSK2981278; GSK 2981278
实验参考方法


1In vitro: GSK2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions.GSK2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK2981278 led to a near-complete inhibition of IL-17A protein secretion.
Reference: Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.
2In vivo: The imiquimod (IMQ) mouse model was employed to demonstrate efficacy of GSK2981278 in a psoriaform-like mouse model. Topical application of IMQ can induce and exacerbate psoriasis-like chronic skin inflammation in mice, including epidermal thickening, a dependence on T cell immunity, and a mechanism dependent on the IL-23/IL-17 pathway. It was first confirmed that GSK2981278 can inhibit IL-17A protein secretion by mouse CD4+ T cells, confirming cross-reactivity of our compound for both mouse and human RORγ (data not shown). Next, mice were treated topically with GSK2981278 (1% ointment or placebo) for three days (day -3 to day 0), after which mice continued to receive compound for the duration of the study. Starting on day 0, mice were challenged topically with IMQ (5%) cream or petrolatum (non-inflammatory inert cream) for up to ten days (day 0 to day +9). On the last day of treatment, the skin was imaged and clinically assessed. GSK2981278 was undetectable (<5 ng/ml) in serum at harvest, indicating that systemic exposure was minimal. Mice exposed to GSK2981278 exhibited reduced skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness when compared to the placebo + IMQ-treated group (Fig 2A and 2B).
Reference: Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.