貨號	規(guī)格	價(jià)格	上海	北京	武漢	南京
S86717-1mg	99.5%	￥355.00 S86717-1mg ￥355.00 現(xiàn)貨	9 9	-	-	-
S86717-5mg	99.5%	￥680.00 S86717-5mg ￥680.00 現(xiàn)貨	9 0 9	-	-	-
S86717-10mg	99.5%	￥1105.00 S86717-10mg ￥1105.00 現(xiàn)貨	13 >10	-	-	-

產(chǎn)品介紹

Pemafibrate is a highly specific PPARα agonist (EC50: 1 nM)

產(chǎn)品描述：

Pemafibrate is a highly specific PPARα agonist (EC50: 1 nM)

靶點(diǎn)：

PPAR

體外研究：

Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ, and h-PPARδ, respectively

體內(nèi)研究：

Pemafibrate (3 mg/kg, p.o.) increases plasma h-apoA-I in human apoA-I (h-apoA-I) transgenic mice, and shows higher levels of plasma h-apoA-I than fenofibrate at 300 mg/kg. Pemafibrate (0.03?mg/kg) decreases levels of triglycerides and aspartate aminotransferase (AST) in PEMA-L (db/db) mice. Pemafibrate (0.1?mg/kg) not only shows such effects but increases liver weight in PEMA-H (db/db) mice. Pemafibrate enhances the pathogenesis in a rodent model of nonalcoholic steatohepatitis (NASH). Pemafibrate significantly reduces the grade of hepatocyte ballooning in PEMA-H mice. Pemafibrate (K-877, 0.0005%) contained in a high-fat diet (HFD) inhibits the body weight gain in mice. Pemafibrate significantly decreases the abundance of triglyceride (TG)-rich lipoproteins, including remnants, in postprandial plasma of mice. Pemafibrate also decreases intestinal mRNA expression of ApoB and Npc1l1

動物實(shí)驗(yàn)：

Mice are fasted for 12?h and fasting blood glucose measured. Nine-week-old db/db mice are used in the assay. After a 2-week acclimatization period, mice are divided into four groups: BD (db/db) mice (fed basal diet (BD) and treated with 0.5% aqueous methylcellulose solution (MC); MCD (db/db) mice (fed methionine choline-deficient (MCD) and treated with 0.5% MC); PEMA-L (db/db) mice (fed MCD and treated with 0.03?mg/kg Pemafibrate); PEMA-H (db/db) mice (fed MCD and treated with 0.1mg/kg Pemafibrate). The drug-free solvent or the dosing solution is administered to animals (5?mL/kg body weight, p.o.) once daily (in the morning) for 4 consecutive weeks. After a 2-week acclimatization period, BD mice are fed a BD for 20 weeks. CTRL mice are fed D09100301 for 20 weeks. PEMA-L and PEMA-H mice are fed D09100301 for 12 weeks followed by D09100301 with 0.4?mg and 1.3?mg Pemafibrate/kg of the diet for 8 weeks, which corresponds to 0.03?mg/kg/day and 0.1mg/kg/day, respectively. FENO mice are fed D09100301 for 12 weeks fo

參考文獻(xiàn)：

1. Yamazaki Y, et al. Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. Epub2007 May 24. 2. Sairyo M, et al. A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb. 2018 Feb 1;25(2):142-152. 3. Honda Y, et al. Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. Sci Rep. 2017 Feb 14;7:42477.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.039 ml	10.193 ml	20.385 ml
5 mM	0.408 ml	2.039 ml	4.077 ml
10 mM	0.204 ml	1.019 ml	2.039 ml
50 mM	0.041 ml	0.204 ml	0.408 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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