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Lanifibranor

Catalog No. T7395 CAS 927961-18-0

Synonyms: IVA337

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

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Lanifibranor, CAS 927961-18-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 213.00
50 mg	In stock	$ 355.00
100 mg	In stock	$ 527.00
500 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.3%

Purity: 98%

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Storage & Solubility Information

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
Targets&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].
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].

Synonyms	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)

References and Literature

1. Ruzehaji N , Frantz C , Ponsoye M , et al. Pan PPAR agonist IVA337 is effective in prevention and treatment of experimental skin fibrosis[J]. Annals of the Rheumatic Diseases, 2016, 75(12):2175-2183. 2. Avouac J , Konstantinova I , Guignabert C , et al. Pan-PPAR agonist IVA337 is effective in experimental lung fibrosis and pulmonary hypertension[J]. Annals of the Rheumatic Diseases, 2017:annrheumdis-2016-210821.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Breast Cancer Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Anti-Cancer Compound Library Anti-Hypertension Compound Library

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Keywords

Lanifibranor 927961-18-0 DNA Damage/DNA Repair Metabolism PPAR Inhibitor inhibit IVA337 Peroxisome proliferator-activated receptors IVA 337 IVA-337 inhibitor

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