Lanifibranor (IVA337) (Synonyms: IVA337) |
| Catalog No.GC31320 |
Lanifibranor (IVA337) 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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 927961-18-0
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[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.
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Animal experiment: |
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]. |
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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. |
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| Cas No. | 927961-18-0 | SDF | |
| Synonyms | IVA337 | ||
| Canonical SMILES | O=C(O)CCCC(N1S(=O)(C2=CC=C3N=CSC3=C2)=O)=CC4=C1C=CC(Cl)=C4 | ||
| Formula | C19H15ClN2O4S2 | M.Wt | 434.92 |
| Solubility | DMSO : 100 mg/mL (229.93 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2993 mL | 11.4964 mL | 22.9927 mL |
| 5 mM | 0.4599 mL | 2.2993 mL | 4.5985 mL |
| 10 mM | 0.2299 mL | 1.1496 mL | 2.2993 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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