Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lanifibranor (IVA337) 是泛过氧化物酶体增殖物激活受体 (PPAR) 激动剂,对人类PPARα,PPARσ和PPARγ的EC50值分别为 1.5, 0.87 和 0.21 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 2,930 | 现货 | ||
100 mg | ¥ 4,260 | 现货 | ||
500 mg | ¥ 8,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | Lanifibranor (IVA337) is an agonist of peroxisome proliferator-activated receptors (PPARs) with EC50 values of 1,537, 866, and 206 nM for human recombinant PPARα, PPARβ, and PPARγ, respectively, for transactivation activity |
靶点活性 | PPARγ:206 nM, PPARβ:866nM , PPARα:1537nM |
体外活性 | In vitro effects of IVA337 included attenuation of transcription of ECM genes and alteration of canonical and non-canonical TGF-β signalling pathways[1]. |
体内活性 | IVA337 demonstrated at a dose of 100 mg/kg a marked protection from the development of lung fibrosis in both mouse models compared with mice receiving 30 mg/kg of IVA337 or vehicle. Histological score was markedly reduced by 61% in the bleomycin model and by 50% in Fra-2 transgenic mice, and total lung hydroxyproline concentrations decreased by 28% and 48%, respectively, as compared with vehicle-treated mice. IVA337 at 100 mg/kg also significantly decreased levels of fibrogenic markers in lesional lungs of both mouse models. In addition, IVA337 substantially alleviated PH in Fra-2 transgenic mice by improving haemodynamic measurements and vascular remodelling. In primary human lung fibroblasts, IVA337 inhibited in a dose-dependent manner fibroblast to myofibroblasts transition induced by TGF-β and fibroblast proliferation mediated by PDGF[2]. |
动物实验 | IVA337 has been evaluated in the mouse model of bleomycin-induced pulmonary fibrosis and in Fra-2 transgenic mice, this latter being characterised by non-specific interstitial pneumonia and severe vascular remodelling of pulmonary arteries leading to PH. Mice received two doses of IVA337 (30 mg/kg or 100 mg/kg) or vehicle administered by daily oral gavage up to 4 weeks[2]. |
别名 | IVA337 |
分子量 | 434.92 |
分子式 | C19H15ClN2O4S2 |
CAS No. | 927961-18-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (229.93 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2993 mL | 11.4964 mL | 22.9927 mL | 57.4818 mL |
5 mM | 0.4599 mL | 2.2993 mL | 4.5985 mL | 11.4964 mL | |
10 mM | 0.2299 mL | 1.1496 mL | 2.2993 mL | 5.7482 mL | |
20 mM | 0.115 mL | 0.5748 mL | 1.1496 mL | 2.8741 mL | |
50 mM | 0.046 mL | 0.2299 mL | 0.4599 mL | 1.1496 mL | |
100 mM | 0.023 mL | 0.115 mL | 0.2299 mL | 0.5748 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Lanifibranor 927961-18-0 DNA Damage/DNA Repair Metabolism PPAR Inhibitor inhibit IVA337 Peroxisome proliferator-activated receptors IVA 337 IVA-337 inhibitor