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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C19H15ClN2O4S2 |
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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 | |||
* <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. |
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. |
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in vitro | IVA337 acts as a pan‐PPAR agonist with moderate and balanced activity on the three PPAR isoforms. IVA337 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. IVA337 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. IVA337 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 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 IVA-337 was evaluated in db/db mice, an obese rodent model of type 2 diabetes characterized by severe insulin resistance, hypertriglyceridemia, marked hyperglycemia. Treatment of db/db mouse with IVA-337 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. IVA-337 has no effect on hematocrit, plasma volume or heart weight. IVA-337 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]. IVA337 normalizes insulin sensitivity while controlling body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning[2]. |
細胞アッセイ | 細胞株 | human primary hepatic stellate cell (hHSC) |
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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 dimethyl sulfoxide 0.1% or a compound (IVA337, 3 µM; rosiglitazone, 3 µM; fenofibrate, 30 µM). hHSC activation was evaluated with western blot by measuring the expression of α‐smooth muscle actin (α-SMA). |
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動物実験 | 動物モデル | C57Bl6 mice |
投薬量 | 10 mg/kg | |
投与方法 | oral |
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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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。