CAS 927961-18-0|Lanifibranor
Introduction：Basic information about CAS 927961-18-0|Lanifibranor, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Lanifibranor | ||
|---|---|---|---|
| CAS Number | 927961-18-0 | Molecular Weight | 434.916 |
| Density | 1.6±0.1 g/cm3 | Boiling Point | 690.9±65.0 °C at 760 mmHg |
| Molecular Formula | C19H15ClN2O4S2 | Melting Point | / |
| MSDS | / | Flash Point | 371.6±34.3 °C |
Names
| Name | Lanifibranor |
|---|---|
| Synonym | More Synonyms |
Lanifibranor BiologicalActivity
| Description | Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively. |
|---|---|
| Related Catalog | Research Areas >>Metabolic Disease |
| Target | PPARγ:206 nM (EC50, Human PPARγ) PPARδ:866 nM (EC50, Human PPARδ) PPARα:1537 nM (EC50, Human PPARα) |
| In Vivo | Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσand PPARγ[1]. Skin fibrosis is attenuated by Lanifibranor (IVA337) (p<0.05, vehicle vs Lanifibranor at 30 mg/kg and p<0.001, vehicle vs Lanifibranor at 100 mg/kg). Both low and high doses of Lanifibranor cause a significant decrease of collagenous matrix deposition. Administration of high (100 mg/kg) doses of Lanifibranor results in reduced body weight compare with vehicle controls (p<0.05; Lanifibranor at 100 mg/kg vs vehicle). Results demonstrate that activation of Peroxisome proliferator-activated receptors (PPARs) with Lanifibranor induces a significant reduction in the infiltration of macrophages, CD45+ leucocytes and lymphocytes in Lanifibranor-treated mice compare with rosiglitazone-treated counterparts[2]. |
| Animal Admin | Male, aged 6 weeks, C57BL/6 mice are used in different animal trials. (i) Experimental dermal fibrosis (preventative model) is induced with bleomycin (n=6 each group). Concurrent treatment with local injections of bleomycin (0.5 mg/mL) and either Lanifibranor (IVA337) (30 mg/kg), Lanifibranor (100 mg/kg) or vehicle by daily oral gavage continued for 3 weeks. (ii) Experimental dermal fibrosis (curative model) is induced using subcutaneous bleomycin for 6 weeks, but 3 weeks after the first injection, mice are given a daily dose of either Lanifibranor (30 mg/kg), Lanifibranor (100 mg/kg) or vehicle by oral gavage for the remaining 3 weeks[2]. |
| References | [1]. Boubia B, et al. Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate. J Med Chem. 2018 Feb 27. [2]. Ruzehaji N, et al. Pan PPAR agonist IVA337 is effective in prevention and treatment of experimental skin fibrosis. Ann Rheum Dis. 2016 Dec;75(12):2175-2183. |
Chemical & Physical Properties
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 690.9±65.0 °C at 760 mmHg |
| Molecular Formula | C19H15ClN2O4S2 |
| Molecular Weight | 434.916 |
| Flash Point | 371.6±34.3 °C |
| Exact Mass | 434.016174 |
| LogP | 4.30 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.727 |
| Storage condition | -20℃ |
Safety Information
| Hazard Codes | N |
|---|
Synonyms
| 4-[1-(1,3-Benzothiazol-6-ylsulfonyl)-5-chloro-1H-indol-2-yl]butanoic acid |
| 28Q8AG0PYL |
| 1H-Indole-2-butanoic acid, 1-(6-benzothiazolylsulfonyl)-5-chloro- |
| lanifibranor |
| IVA-337 |
