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GSK2981278

Name: GSK2981278
Brand: TargetMol
SKU: T4050
Price: 333 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.67%

货号 T4050Cas号 1474110-21-8

别名 ROR gama modulator 1

GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活，并且干扰 RORγ-DNA 结合。

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GSK2981278

一键复制产品信息

很棒

纯度: 99.67%

货号 T4050 别名 ROR gama modulator 1Cas号 1474110-21-8

GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活，并且干扰 RORγ-DNA 结合。

规格	价格	库存
1 mg	¥ 333	现货
2 mg	¥ 482	现货
5 mg	¥ 759	现货
10 mg	¥ 1,130	现货
25 mg	¥ 2,260	现货
50 mg	¥ 3,390	现货
100 mg	¥ 4,930	现货
500 mg	¥ 9,870	现货
1 mL x 10 mM (in DMSO)	¥ 798	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

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资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

生物活性

产品描述	GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
别名	ROR gama modulator 1

化学信息

分子量	461.61
分子式	C₂₅H₃₅NO₅S
CAS No.	1474110-21-8
Smiles	CCc1ccc(cc1)N(CC(C)C)S(=O)(=O)c1ccc(OCC2CCOCC2)c(CO)c1
密度	1.180 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 50 mg/mL (108.32 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.33 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1663 mL	10.8317 mL	21.6633 mL	108.3165 mL
5 mM	0.4333 mL	2.1663 mL	4.3327 mL	21.6633 mL
10 mM	0.2166 mL	1.0832 mL	2.1663 mL	10.8317 mL
20 mM	0.1083 mL	0.5416 mL	1.0832 mL	5.4158 mL
50 mM	0.0433 mL	0.2166 mL	0.4333 mL	2.1663 mL
100 mM	0.0217 mL	0.1083 mL	0.2166 mL	1.0832 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20g，给药体积100 μL， TargetMol | Animal experiments

一共给药动物10只，您使用的配方为5% TargetMol | reagent

DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline /PBS/ddH₂O，那么您的工作液浓度为2mg/mL。

母液配置方法: 2 mg 药物溶于 50 μLDMSO TargetMol | reagent

（母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法: 取 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline /PBS/ddH₂O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

TargetMol AI Summary

GSK2981278 is a multifaceted bioactive molecule exhibiting notable high lipophilicity with a LogD value of 5.9. It demonstrates potent inverse agonist activity against the RORgamma receptor, with IC50 values ranging from 10.0 nM to 30.0 nM in various assays, including human Jurkat cells and human HeLa-derived HG5LN cells. The compound shows significant metabolic stability in human liver microsomes, displaying a short half-life of 0.01333 hours and high intrinsic clearance of 1613.9 mL.min-1.kg-1. In addition, GSK2981278 has demonstrated inhibitory activity against the SARS-CoV-2 3CL-Pro protease, achieving an inhibition percentage of 23.09% at a concentration of 20 µM. It also reduces SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10 µM concentration, although with a relatively low inhibition rate of -0.06%. Its anti-inflammatory efficacy is highlighted in an imiquimod-induced mouse model of psoriasis, showing a 64.3% reduction in clinical scores when applied topically. In human ex-vivo studies, the compound significantly reduces proinflammatory cytokines such as IL-17A, IL-17F, IL-22, and IL-19 by more than 50%. Furthermore, GSK2981278 promotes cell viability in various cell lines, such as HEK293T and U2OS cells, with a mixed effect on growth rates. It also exhibits a modulatory effect on protein stability in different domains, as indicated by varying thermal shift assay results. Overall, GSK2981278 presents a robust profile of activity across inflammatory, antiviral, and immunomodulatory pathways, promising for further therapeutic developments..

Note: Summary generated by AI, AI may be wrong some times, we do not provide any medical advice and only sell our product to accredited institution, Please cross-check with other sources, data source: chembl