Home Metabolism PPAR agonist Lanifibranor (IVA-337) For research use only.

Lanifibranor (IVA-337)

Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.

Lanifibranor (IVA-337) Chemical Structure

Lanifibranor (IVA-337) Chemical Structure

CAS No. 927961-18-0

Purity & Quality Control

Lanifibranor (IVA-337) Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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
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Biological Activity

Description Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.
Targets
PPARγ [1] PPARδ [1] PPARα [1]
206 nM(EC50) 866 nM(EC50) 1537 nM(EC50)
In vitro
In vitro

IVA337 acts as a pan‐PPAR agonist with moderate and balanced activity on the three PPAR isoforms. IVA337 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. IVA337 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. IVA337 inhibits PDGF-induced proliferation, stiffness-induced activation, and TGF-β1-induced overexpression of fibrotic genes in hHSCs (human primary hepatic stellate cells)[2].
Cell Research Cell lines human primary hepatic stellate cell (hHSC)
Concentrations 3 μM
Incubation Time 7 days
Method

Human primary HSCs were seeded on plastic six-well plates for 7 days in complete medium with either DMSO 0.1% or a compound (IVA337, 3 µM). hHSC activation was evaluated with western blot by measuring the expression of α‐smooth muscle actin (α-SMA).
In Vivo
In vivo

Following a single oral dose (10 mg/kg in methyl cellulose as vehicle) of 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 IVA-337 was evaluated in db/db mice, an obese rodent model of type 2 diabetes, hypertriglyceridemia, marked hyperglycemia. Treatment of db/db mouse with IVA-337 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. IVA-337 has no effect on hematocrit, plasma volume or heart weight. IVA-337 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[1]. IVA337 controlled body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning[2].
Animal Research Animal Models C57Bl6 mice
Dosages 10 mg/kg
Administration oral
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

Chemical Information & Solubility

Molecular Weight 434.92 Formula

C19H15ClN2O4S2
CAS No. 927961-18-0 SDF --
Smiles C1=CC2=C(C=C1S(=O)(=O)N3C4=C(C=C(C=C4)Cl)C=C3CCCC(=O)O)SC=N2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (200.03 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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