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GSK3787 96%

GSK3787

源葉(MedMol)
S80498
188591-46-0
C15H12ClF3N2O3S
392.78
MFCD00099612
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫存（上海） 北京 武漢 南京 購買數(shù)量
源葉(MedMol) S80498-5mg 96% ￥90.00元 3 - - -
源葉(MedMol) S80498-10mg 96% ￥130.00元 7 - - -
源葉(MedMol) S80498-25mg 96% ￥280.00元 7 - - -
源葉(MedMol) S80498-50mg 96% ￥500.00元 4 - - -
源葉(MedMol) S80498-100mg 96% ￥950.00元 預(yù)計(jì)交期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
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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