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GSK2981278 {[allProObj[0].p_purity_real_show]}

货号:A576988

GSK2981278 is a retinoid-related orphan receptor gamma (RORy) modulator.

GSK2981278 化学结构 CAS号:1474110-21-8
GSK2981278 化学结构
CAS号:1474110-21-8
GSK2981278 3D分子结构
CAS号:1474110-21-8
GSK2981278 化学结构 CAS号:1474110-21-8
GSK2981278 3D分子结构 CAS号:1474110-21-8
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GSK2981278 纯度/质量文件 产品仅供科研

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GSK2981278 生物活性

描述 GSK2981278 is recognized as a potent and selective inverse agonist of RORγ, effectively inhibiting the activation of the IL17 promoter and disrupting RORγ-DNA binding[1].
体内研究

Topical application of GSK2981278 (1% in ointment; for three days) results in a reduction of skin redness and scaling, along with a 23% reduction in epidermal thickness, indicating its effectiveness in attenuating inflammation in a mouse model of psoriasis[1].

体外研究

GSK2981278 significantly suppresses IL-17A and IL-22 protein secretion in a concentration-dependent manner with an IC50 of 3.2 nM, especially noticeable during 5 days of culture under Th17 skewing conditions[1].

At varying concentrations (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; over 5 days), GSK2981278 shows potent and selective inhibition of IL-17 and IL-22 levels, with concentrations ≥3 nM leading to nearly complete inhibition of IL-17A protein secretion[1].

GSK2981278 参考文献

[1]Smith SH, et al. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979.

GSK2981278 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.66mL

4.33mL

2.17mL

GSK2981278 技术信息

CAS号1474110-21-8
分子式C25H35NO5S
分子量 461.614
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(227.46 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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