Lanifibranor (IVA-337)

Catalog No.S8770

For research use only.

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

CAS No. 927961-18-0

Selleck's Lanifibranor (IVA-337) has been cited by 1 Publication

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 M{PQcGZ2dmO2aX;uJIF{e2G7 MXzUdoFve2GldHn2ZZRqd25ib3[gcY92e2ViR1HMOE1nfXOnZDDQVGFT\2GvbXGgUGJFKGW6cILld5Nm\CCrbjDB[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGOxLXX4dJJme3OrbnegOWdidDRicFfMN{BVUyCOdXOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMkCy{txO MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2Nkm0Nkc,Ojl2NE[5OFI9N2F-
COS7 Mn60SpVv[3Srb36gZZN{[Xl? NI\lTldVemGwc3HjeIl3[XSrb36gc4YhcHWvYX6gS2FNPC2odYPl[EBRWEGUZ3HtcYEhVEKGIHX4dJJme3OnZDDpckBC\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHPvMYV5eHKnc4PpcochPUejbESgdGdNOyCWSzDMeYMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNlA3|ryP NHnMXHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS0Olk1Oid-Mkm0OFY6PDJ:L3G+
COS7 NVH5ZnNHTnWwY4Tpc44h[XO|YYm= NHrm[I9VemGwc3HjeIl3[XSrb36gc4YhdW:3c3WgS2FNPC2odYPl[EBRWEGUYXzwbIEhVEKGIHX4dJJme3OnZDDpckBC\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHPvMYV5eHKnc4PpcochPUejbESgdGdNOyCWSzDMeYMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuN|Y3|ryP NUD4ZXJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFY6PDJpPkK5OFQ3QTR{PD;hQi=>
COS7 MkfrSpVv[3Srb36gZZN{[Xl? MVfUdoFve2GldHn2ZZRqd25ib3[gbJVu[W5iR1HMOE1nfXOnZDDQVGFT\GWudHGgUGJFKGW6cILld5Nm\CCrbjDB[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGOxLXX4dJJme3OrbnegOWdidDRicFfMN{BVUyCOdXOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwOE[2{txO M4q0PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NES2PVQzLz5{OUS0Olk1OjxxYU6=
COS7 NGfY[YxHfW6ldHnvckBie3OjeR?= MYHUdoFve2GldHn2ZZRqd25ib3[gbJVu[W5iR1HMOE1nfXOnZDDQVGFT[WyyaHGgUGJFKGW6cILld5Nm\CCrbjDB[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGOxLXX4dJJme3OrbnegOWdidDRicFfMN{BVUyCOdXOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTFwNUO3{txO Mn72QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NE[5OFIoRjJ7NES2PVQzRC:jPh?=
COS7 M1L1NmZ2dmO2aX;uJIF{e2G7 NILCOZBVemGwc3HjeIl3[XSrb36gc4YhdW:3c3WgS2FNPC2odYPl[EBRWEGUZHXseIEhVEKGIHX4dJJme3OnZDDpckBC\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHPvMYV5eHKnc4PpcochPUejbESgdGdNOyCWSzDMeYMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUGuOVbPxE1? NXPScZZ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFY6PDJpPkK5OFQ3QTR{PD;hQi=>
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 characterized by severe insulin resistance, 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 normalizes insulin sensitivity while controlling body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning[2].

Protocol (from reference)

Cell Research:

[2]

  • 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 dimethyl sulfoxide 0.1% or a compound (IVA337, 3 µM; rosiglitazone, 3 µM; fenofibrate, 30 µM; or GW501516, 3 µM). hHSC activation was evaluated with western blot by measuring the expression of α‐smooth muscle actin (α-SMA).

Animal Research:

[1]

  • Animal Models: C57Bl6 mice
  • Dosages: 10 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 434.92
Formula

C19H15ClN2O4S2

CAS No. 927961-18-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC2=C(C=C1S(=O)(=O)N3C4=C(C=C(C=C4)Cl)C=C3CCCC(=O)O)SC=N2

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03866369 Completed Drug: Moxifloxacin|Drug: Placebo|Drug: Lanifibranor Healthy Subjects Inventiva Pharma|Parexel January 17 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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