Name: Lanifibranor (IVA-337)
Brand: Selleck Chemicals
SKU: S8770
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.59%

99.59

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PPAR Inhibitors	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 Harmine Astaxanthin Eupatilin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
COS7	Function assay	Transactivation of mouse GAL4-fused PPARgamma LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=0.202μM	29446942
COS7	Function assay	Transactivation of human GAL4-fused PPARgamma LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=0.206μM	29446942
COS7	Function assay	Transactivation of mouse GAL4-fused PPARalpha LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=0.366μM	29446942
COS7	Function assay	Transactivation of human GAL4-fused PPARdelta LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=0.866μM	29446942
COS7	Function assay	Transactivation of human GAL4-fused PPARalpha LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=1.537μM	29446942
COS7	Function assay	Transactivation of mouse GAL4-fused PPARdelta LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay, EC50=1.56μM	29446942
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	434.92	Formula	C₁₉H₁₅ClN₂O₄S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	927961-18-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC2=C(C=C1S(=O)(=O)N3C4=C(C=C(C=C4)Cl)C=C3CCCC(=O)O)SC=N2

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (200.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	PPARγ 206 nM(EC50) PPARδ 866 nM(EC50) PPARα 1537 nM(EC50)
In vitro	Lanifibranor (IVA-337) acts as a pan‐PPAR agonist with moderate and balanced activity on the three PPAR isoforms. Its 50% effective concentration (EC50) levels for the human PPARs (hPPARs) were 1.63E-06 M for PPARα, 8.49E-07 M for PPARδ, and 2.28E-07 M for PPARγ. This compound's EC50 levels for the rodent PPARs were 3.78E-07 M for PPARα, 1.55E-06 M for PPARδ, and 2.23E-07 M for PPARγ. It inhibits PDGF-induced proliferation, stiffness-induced activation, and TGF-β1-induced overexpression of fibrotic genes in hHSCs (human primary hepatic stellate cells).
In vivo	Following a single oral dose (10 mg/kg in methyl cellulose as vehicle) of Lanifibranor (IVA-337) in C57Bl6 mice, plasma pharmacokinetic parameters are evaluated. The Cmax, Tmax and AUCinf are 10710 ng/mL, 1 h and 29367 h·(ng/mL), respectively. The anti-diabetic effect of this compound was evaluated in db/db mice, an obese rodent model of type 2 diabetes, hypertriglyceridemia, marked hyperglycemia. Treatment of db/db mouse with it for 5 days induces a dose dependent and significant decrease of circulating glucose levels: 40% at 10 mg/kg, and 58% at 30 mg/kg. In the same study abnormal plasma triglycerides levels observed in this disease model were markedly corrected following treatment with IVA-337: 33% at 10 mg/kg, and 45% at 30 mg/kg. It has no effect on hematocrit, plasma volume or heart weight. This compound demonstrates excellent anti-hyperglycemic and hypolipidemic efficacy in the db/db mouse model, and a significant anti-fibrotic activity in the mouse CCl4-induced liver fibrosis model. It controlled body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29446942/ [2] https://pubmed.ncbi.nlm.nih.gov/29404476/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05232071	Active not recruiting	NASH - Nonalcoholic Steatohepatitis\|Diabetes Mellitus Type 2	Inventiva Pharma	June 29 2022	Phase 2
NCT03866369	Completed	Healthy Subjects	Inventiva Pharma\|Parexel	January 17 2019	Phase 1

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Lanifibranor (IVA-337) PPAR agonist

Chemical Structure

Molecular Weight: 434.92