Lanifibranor (IVA-337)

製品コードS8770 バッチS877001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C19H15ClN2O4S2
分子量 434.92 CAS No. 927961-18-0
Solubility (25°C)* 体外 DMSO 87 mg/mL (200.03 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (11.50mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.
in vitro

Lanifibranor (IVA-337) acts as a pan‐PPAR agonist with moderate and balanced activity on the three PPAR isoforms. Its 50% effective concentration (EC50) levels for the human PPARs (hPPARs) were 1.63E-06 M for PPARα, 8.49E-07 M for PPARδ, and 2.28E-07 M for PPARγ. This compound's EC50 levels for the rodent PPARs were 3.78E-07 M for PPARα, 1.55E-06 M for PPARδ, and 2.23E-07 M for PPARγ. It inhibits PDGF-induced proliferation, stiffness-induced activation, and TGF-β1-induced overexpression of fibrotic genes in hHSCs (human primary hepatic stellate cells)[2].
in vivo

Following a single oral dose (10 mg/kg in methyl cellulose as vehicle) of Lanifibranor (IVA-337) in C57Bl6 mice, plasma pharmacokinetic parameters are evaluated. The Cmax, Tmax and AUCinf are 10710 ng/mL, 1 h and 29367 h·(ng/mL), respectively. The anti-diabetic effect of this compound was evaluated in db/db mice, an obese rodent model of type 2 diabetes, hypertriglyceridemia, marked hyperglycemia. Treatment of db/db mouse with it for 5 days induces a dose dependent and significant decrease of circulating glucose levels: 40% at 10 mg/kg, and 58% at 30 mg/kg. In the same study abnormal plasma triglycerides levels observed in this disease model were markedly corrected following treatment with IVA-337: 33% at 10 mg/kg, and 45% at 30 mg/kg. It has no effect on hematocrit, plasma volume or heart weight. This compound demonstrates excellent anti-hyperglycemic and hypolipidemic efficacy in the db/db mouse model, and a significant anti-fibrotic activity in the mouse CCl4-induced liver fibrosis model[1]. It controlled body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human primary hepatic stellate cell (hHSC)
濃度 3 μM
反応時間 7 days
実験の流れ

Human primary HSCs were seeded on plastic six-well plates for 7 days in complete medium with either DMSO 0.1% or Lanifibranor (IVA-337) at 3 µM. hHSC activation was evaluated with western blot by measuring the expression of α‐smooth muscle actin (α-SMA).
動物実験 動物モデル C57Bl6 mice
投薬量 10 mg/kg
投与方法 oral

参考

  • https://pubmed.ncbi.nlm.nih.gov/29446942/
  • https://pubmed.ncbi.nlm.nih.gov/29404476/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inhibition of adenosine/A2A receptor signaling suppresses dermal fibrosis by enhancing fatty acid oxidation [ Cell Commun Signal, 2025, 23(1):206] PubMed: 40301970
Antidepressant-like actions of lanifibranor and its related mechanisms in mouse models of depression: Involvement of hippocampal PPARα and BDNF [ Biomed Pharmacother, 2025, 191:118406] PubMed: 40840108
Berberine exerts neuroprotective activities against cerebral ischemia/reperfusion injury through up-regulating PPAR-γ to suppress NF-κB-mediated pyroptosis [ Brain Res Bull, 2021, 177:22-30] PubMed: 34517069

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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