S80498 |
GSK3787 |
源葉(MedMol) | 96% |
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- 產(chǎn)品描述: GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
- 靶點(diǎn): PPARδ:6.6 nM (pIC50);PPAR
- 體內(nèi)研究:
GSK3787 has pharmacokinetic properties suitable for use as an in vivo PPARδ antagonist tool compound in mice. GSK3787 is 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 (Vss) following iv administration are 39±11 (mL/min)/kg and 1.7±0.4 L/kg, respectively. Following oral administration, good exposure (Cmax=881±166 ng/mL, AUCinf=3343±332 h?ng/mL), half-life (2.7±1.1 h), and bioavailability (F=77±17%) are observed. Oral administration of GSK3787 (10 mg/kg) leads to a serum Cmax?of 2.2±0.4 μM in C57BL/6 male mice. Oral administration of GW0742 causes an increase in expression of Angptl4 and Adrp mRNA (known PPARβ/δ target genes) in wild-type mouse colon epithelium, and this effect is not found in?Pparβ/δ-null mouse colon epithelium. Coadministration of GSK3787 with GW0742 effectively prevents the ligand-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, and this effect is not found in?Pparβ/δ-null mouse colon epithelium. Oral administration of GSK3787 causes a modest increase in promoter occupancy of PPARβ/δ in the PPRE region of both the?Angptl4?and?Adrp?genes, but coadministration of GSK3787 with GW0742 results in markedly less accumulation of PPARβ/δ in the PPRE region of both the?Angptl4?and?Adrp?genes in wild-type mouse colon epithelium
- 參考文獻(xiàn):
1. Shearer BG, 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. 20 2. Palkar PS, et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010 Sep;78(3):419-30.
- 溶解性: DMSO : ≥ 50 mg/mL (127.30 mM)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.546 ml 12.73 ml 25.46 ml 5 mM 0.509 ml 2.546 ml 5.092 ml 10 mM 0.255 ml 1.273 ml 2.546 ml 50 mM 0.051 ml 0.255 ml 0.509 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)