GSK3787
(Synonyms: GSK-3787,GSK 3787) 目录号 : GC16009
A selective, irreversible PPARβ/δ antagonist
Cas No.:188591-46-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK3787 is a novel and irreversible antagonist of the peroxisome proliferator-activated receptor-β/δ (PPAR-β/δ) that covalently binds to a cysteine residue in the ligand-binding domain of PPAR- β/δ. Although it responses to ligand activation to modulate the association of both PPAR-β/δ and PPAR-γ coregulator peptides, GSK3787 exhibits considerably higher antagonism of PPAR-β/δ than that of PPAR-γ. Results of recent studies have shown that oral administration of GSK3787 results in the antagonism of GW0742-induced overexpression of Angptl4 and Adrp mRNA in wild-type mouse colon, which is correlated with reduced promoter occupancy of PPAR-β/δ on the Angptl4 and Adrp genes.
Reference
[1].Palkar PS, Borland MG, Naruhn S, Ferry CH, Lee C, Sk UH, Sharma AK, Amin S, Murray IA, Anderson CR, Perdew GH, Gonzalez FJ, Müller R, Peters JM. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010;78(3):419-430
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.546 mL | 12.7298 mL | 25.4595 mL |
| 5 mM | 0.5092 mL | 2.546 mL | 5.0919 mL |
| 10 mM | 0.2546 mL | 1.273 mL | 2.546 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。