Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 22,500 | |||
25 mg | 在庫あり | ¥ 49,000 | |||
50 mg | 在庫あり | ¥ 81,500 | |||
100 mg | 在庫あり | ¥ 121,000 | |||
500 mg | 在庫あり | ¥ 259,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 14,000 |
説明 | 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 |
ターゲット&IC50 | PPARγ:206 nM, PPARβ:866nM , PPARα:1537nM |
In vitro | In vitro effects of IVA337 included attenuation of transcription of ECM genes and alteration of canonical and non-canonical TGF-β signalling pathways[1]. |
In vivo | 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]. |
動物実験 | 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]. |
別名 | 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)
You can also refer to dose conversion for different animals. 詳細
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Lanifibranor 927961-18-0 DNA Damage/DNA Repair Metabolism PPAR Inhibitor inhibit IVA337 Peroxisome proliferator-activated receptors IVA 337 IVA-337 inhibitor