Lanifibranor (IVA-337)

For research use only.

Catalog No.S8770

Lanifibranor (IVA-337) Chemical Structure

CAS No. 927961-18-0

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.

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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 NF[yR5hHfW6ldHnvckBie3OjeR?= M{TMcXRz[W6|YXP0bZZifGmxbjDv[kBud3W|ZTDHRWw1NW[3c3XkJHBRSVKpYX3tZUBNSkRiZYjwdoV{e2WmIHnuJGFnemmlYX6g[5Jm\W5ibX;ub4V6KEORU{egZ4VtdHNiY3:t[ZhxemW|c3nu[{A2T2GuNDDwS2w{KFSNIFz1Z{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6yNFLPxE1? MlzjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NE[5OFIoRjJ7NES2PVQzRC:jPh?=
COS7 M2n5eGZ2dmO2aX;uJIF{e2G7 NVzOUIhuXHKjboPhZ5RqfmG2aX;uJI9nKGi3bXHuJGdCVDRvZoXz[YQhWFCDUnfhcY1iKEyERDDlfJBz\XO|ZXSgbY4hSW[{aXPhckBoemWnbjDtc45s\XliQ1;TO{Bk\WyuczDjc{1mgHC{ZYPzbY5oKDWJYXy0JJBIVDNiVFugUJVkKGGodHXyJI93\XKwaXfoeEBqdmO3YnH0bY9vKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlIxPs7:TR?= NYLoUG5jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFY6PDJpPkK5OFQ3QTR{PD;hQi=>
COS7 M3q3fmZ2dmO2aX;uJIF{e2G7 MVvUdoFve2GldHn2ZZRqd25ib3[gcY92e2ViR1HMOE1nfXOnZDDQVGFT[WyyaHGgUGJFKGW6cILld5Nm\CCrbjDB[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGOxLXX4dJJme3OrbnegOWdidDRicFfMN{BVUyCOdXOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwM{[2{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2Nkm0Nkc,Ojl2NE[5OFI9N2F-
COS7 MmH5SpVv[3Srb36gZZN{[Xl? M13rWXRz[W6|YXP0bZZifGmxbjDv[kBpfW2jbjDHRWw1NW[3c3XkJHBRSVKmZXz0ZUBNSkRiZYjwdoV{e2WmIHnuJGFnemmlYX6g[5Jm\W5ibX;ub4V6KEORU{egZ4VtdHNiY3:t[ZhxemW|c3nu[{A2T2GuNDDwS2w{KFSNIFz1Z{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD64OlbPxE1? NHfGbZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS0Olk1Oid-Mkm0OFY6PDJ:L3G+
COS7 M3PY[2Z2dmO2aX;uJIF{e2G7 NIPxOm9VemGwc3HjeIl3[XSrb36gc4YhcHWvYX6gS2FNPC2odYPl[EBRWEGUYXzwbIEhVEKGIHX4dJJme3OnZDDpckBC\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHPvMYV5eHKnc4PpcochPUejbESgdGdNOyCWSzDMeYMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUGuOVM4|ryP NYL5Z25[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFY6PDJpPkK5OFQ3QTR{PD;hQi=>
COS7 Mm\oSpVv[3Srb36gZZN{[Xl? M4LFW3Rz[W6|YXP0bZZifGmxbjDv[kBud3W|ZTDHRWw1NW[3c3XkJHBRSVKmZXz0ZUBNSkRiZYjwdoV{e2WmIHnuJGFnemmlYX6g[5Jm\W5ibX;ub4V6KEORU{egZ4VtdHNiY3:t[ZhxemW|c3nu[{A2T2GuNDDwS2w{KFSNIFz1Z{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MT61Ou69VQ>? MmH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NE[5OFIoRjJ7NES2PVQzRC:jPh?=

... Click to View More Cell Line Experimental Data

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

Cell Research:

[2]

- Collapse
  • 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).


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: C57Bl6 mice
  • Dosages: 10 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (200.03 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 434.92
Formula

C19H15ClN2O4S2

CAS No. 927961-18-0
Storage powder
in 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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID