GSK2981278
目录号 : GC13905
An inverse agonist of RORγ
Cas No.:1474110-21-8
Sample solution is provided at 25 µL, 10mM.
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GSK2981278 is a RORγ-selective inverse agonist.
RAR-related orphan receptor gamma (RORγ) is a protein that in humans is encoded by the RORC gene. The RORγ protein is a DNA-binding transcription factor and is a member of the NR1 subfamily of nuclear receptors.
In vitro: Previous study found that GSK2981278 had no significant effect on RORα-dependent activation, indicating its selectivity for RORγ. GSK2981278 also demonstrated 10-fold greater potency for IL-17A inhibition than its analogs of GSK3038548 and GSK3038549. In addition, authors examined the effect of GSK2981278 on endogenous il17a expression in Jurkat cells. Results showed that GSK2981278 could repress the activation of il17a by RORγt in a dose-responsive manner [1].
In vivo: In previous study, the imiquimod (IMQ) mouse model was employed to demonstrate efficacy of GSK2981278 in a psoriaform-like mouse model. Results showed that the topical application of IMQ could induce and exacerbate psoriasis-like chronic skin inflammation in mice. Next, mice were treated topically with GSK2981278 for three days, after which mice continued to receive compound for the duration of the study. It was found that GSK2981278 was undetectable in serum at harvest, suggesting that systemic exposure was minimal. In addition, mice exposed to GSK2981278 exhibited reduced skin redness and scaling, as well as decreased hyperplasia [1].
Clinical trial: The study of safety and efficacy of topical GSK2981278 ointment in plaque psoriasis has been finished but there is no results released [2].
References:
[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.
[2] https://clinicaltrials. gov/ct2/show/NCT02548052 term=GSK2981278&rank=2
| Cas No. | 1474110-21-8 | SDF | |
| 化学名 | N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide | ||
| Canonical SMILES | OCC1=CC(S(N(CC(C)C)C2=CC=C(CC)C=C2)(=O)=O)=CC=C1OCC3CCOCC3 | ||
| 分子式 | C25H35NO5S | 分子量 | 461.6 |
| 溶解度 | ≤15mg/ml in ethanol;5mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1664 mL | 10.8319 mL | 21.6638 mL |
| 5 mM | 0.4333 mL | 2.1664 mL | 4.3328 mL |
| 10 mM | 0.2166 mL | 1.0832 mL | 2.1664 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet