• 提示：詳情請(qǐng)下載說明書。

• 產(chǎn)品描述： Elafibranor (GFT505) 是PPAR-alpha和PPAR-δ的激動(dòng)劑，改善胰島素敏感度、有益于葡萄糖穩(wěn)態(tài)、脂質(zhì)代謝并減少炎癥

• 靶點(diǎn)： PPARα; PPARδ ;PPAR

• 體外研究：
  GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ

• 體內(nèi)研究：
  Elafibranor (GFT505) is a dual PPARα/δ agonist that has demonstrated efficacy in disease models of nonalcoholic fatty liver disease (NAFLD)/NASH and liver fibrosis. In the rat, GFT505 concentrated in the liver with limited extrahepatic exposure and underwent extensive enterohepatic cycling. Elafibranor confers liver protection by acting on several pathways involved in NASH pathogenesis, reducing steatosis, inflammation, and fibrosis. GFT505 improved liver dysfunction markers, decreased hepatic lipid accumulation, and inhibited proinflammatory (interleukin-1 beta, tumor necrosis factor alpha, and F4/80) and profibrotic (transforming growth factor beta, tissue inhibitor of metalloproteinase 2, collagen type I, alpha 1, and collagen type I, alpha 2) gene expression

• 細(xì)胞實(shí)驗(yàn)： Cell lines: hSKP-HPCs Concentrations: 30 μM Incubation Time: 24 h Method: Cells were treated with indicated concentration of drug for 24 h.

• 動(dòng)物實(shí)驗(yàn)： Animal Models: hApoE2 KI and hApoE2 KI/PPAR-α KO mice Dosages: 30 mg/kg Administration: oral gavage

• 參考文獻(xiàn)：
  1. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016, 150(5):1147-1159.e5. 2. Staels B, et al. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis. Hepatology. 2013, 58(6):1941-52. 3. Boeckmans J, et al. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH. Pharmacol Res. 2019 Jun;144:377-389.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.601 ml	13.004 ml	26.009 ml
  5 mM	0.52 ml	2.601 ml	5.202 ml
  10 mM	0.26 ml	1.3 ml	2.601 ml
  50 mM	0.052 ml	0.26 ml	0.52 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。

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)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *