188591-46-0|GSK3787|CsnPharm

CAS No.: 188591-46-0

GSK3787 Catalog No. CSN15822

Synonyms: GSK3787

GSK3787 selectively and irreversibly antagonizes PPARδ with pIC50 of 6.6 with no significant effect on hPPARα or hPPARγ.

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技术信息

生物活性

描述The peroxisome proliferator-activated receptors (PPARs) are ligand activated transcription factors belonging to the nuclear receptor superfamily and play key roles in multiple physiological pathway. Three PPAR receptor subtypes, designated as PPARα, PPARγ, and PPARδ, have been identified. PPARδ is recognized as a regulator of genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. GSK3787 is a potent and selective antagonist for PPARδ with pIC₅₀ value of 6.6 in ligand displacement assay. GSK3787 completely antagonized the activity of PPARδ agonist 1 with a pIC₅₀ of 6.9. GSK3787 was administered to human skeletal muscle cells at various doses and found to effectively antagonize the gene expression of CPT1a. This suggests that GSK3787 may selectively block the basal activity of the receptor on some PPARδ target genes highlighting the potential utility of this compound as a useful tool for further elucidating the biological role of PPARδ. GSK3787 was administered intravenously (0.5 mg/kg) and orally (10 mg/kg) to male C57BL/6 mice. Mean clearance (CL) and volume of distribution at steady state (V_ss) following iv administration were 39 ± 11 (mL/min)/kg and 1.7 ± 0.4 L/kg, respectively. Following oral administration, good exposure (C_max = 881 ± 166 ng/mL, AUC_inf = 3343 ± 332 hng/mL), half-life (2.7 ± 1.1 h), and bioavailability (F = 77 ± 17%) were observed. Thus, GSK3787 has pharmacokinetic properties suitable for use as an in vivo PPARδ antagonist tool compound in mice^[1].
作用机制GSK3787 covalently modifies Cys249 within the ligand binding pocket^[1].
参考文献

[1] Shearer BG, Wiethe RW, Ashe A, et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010;53(4):1857-1861.
[2] Palkar PS, Borland MG, et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010 Sep;78(3):419-30.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5460 mL
- 12.7298 mL
- 25.4595 mL
- 5 mM
- 0.5092 mL
- 2.5460 mL
- 5.0919 mL
- 10 mM
- 0.2546 mL
- 1.2730 mL
- 2.5460 mL

技术信息

CAS号

188591-46-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12ClF3N2O3S

运输

蓝冰

分子量

392.78

别名

GSK3787

溶解度

DMSO	190.0 mg/mL (483.7 mM)
Water	insoluble

动物实验配方

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