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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $55 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $213 | In Stock | |
50 mg | $355 | In Stock | |
100 mg | $527 | In Stock | |
500 mg | $1,130 | In Stock | |
1 mL x 10 mM (in DMSO) | $61 | In Stock |
Description | 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 |
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]. |
Animal Research | 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]. |
Alias | IVA337 |
Molecular Weight | 434.92 |
Formula | C19H15ClN2O4S2 |
Cas No. | 927961-18-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (229.93 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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