Lanifibranor | IVA-337 | CAS#927961-18-0 | PARP agonist

MedKoo Cat#: 329504 | Name: Lanifibranor

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.

Chemical Structure

Lanifibranor

CAS#927961-18-0

Theoretical Analysis

MedKoo Cat#: 329504

Name: Lanifibranor

CAS#: 927961-18-0

Chemical Formula: C19H15ClN2O4S2

Exact Mass: 434.0162

Molecular Weight: 434.91

Elemental Analysis: C, 52.47; H, 3.48; Cl, 8.15; N, 6.44; O, 14.71; S, 14.74

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
500mg	USD 2,950.00	2 Weeks

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Related CAS #

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Synonym

Lanifibranor; IVA-337; IVA 337; IVA337.

IUPAC/Chemical Name

4-(1-(1,3-Benzothiazol-6-ylsulfonyl)-5-chloro-indol-2-yl)butanoic acid

InChi Key

OQDQIFQRNZIEEJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H15ClN2O4S2/c20-13-4-7-17-12(8-13)9-14(2-1-3-19(23)24)22(17)28(25,26)15-5-6-16-18(10-15)27-11-21-16/h4-11H,1-3H2,(H,23,24)

SMILES Code

O=C(O)CCCC(N1S(=O)(C2=CC=C3N=CSC3=C2)=O)=CC4=C1C=CC(Cl)=C4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

In primary human lung fibroblasts, IVA337 inhibited in a dose-dependent manner fibroblast to myofibroblasts transition induced by TGF-β and fibroblast proliferation mediated by PDGF. Reference: Ann Rheum Dis. 2017 Nov;76(11):1931-1940. https://pubmed.ncbi.nlm.nih.gov/28801346/

In vivo activity:

IVA337 normalized insulin sensitivity while controlling body weight gain, adiposity index, and serum triglyceride increases; it decreased liver steatosis, inflammation, and ballooning in mice. IVA337 demonstrated preventive and curative effects on fibrosis in the CCl4 model and inhibited proliferation and activation of human hepatic stellate cells, the key cells driving liver fibrogenesis in NASH. Reference: Hepatol Commun. 2017 Jun 19;1(6):524-537. https://pubmed.ncbi.nlm.nih.gov/29404476/

	Solvent	mg/mL	mM
Solubility
	DMF	50.0	114.97
	DMSO	79.0	181.65
	DMSO:PBS (pH 7.2) (1:4)	0.2	0.46
	Ethanol	0.2	0.46

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 434.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Avouac J, Konstantinova I, Guignabert C, Pezet S, Sadoine J, Guilbert T, Cauvet A, Tu L, Luccarini JM, Junien JL, Broqua P, Allanore Y. Pan-PPAR agonist IVA337 is effective in experimental lung fibrosis and pulmonary hypertension. Ann Rheum Dis. 2017 Nov;76(11):1931-1940. doi: 10.1136/annrheumdis-2016-210821. Epub 2017 Aug 11. PMID: 28801346. 2. Boyer-Diaz Z, Aristu-Zabalza P, Andrés-Rozas M, Robert C, Ortega-Ribera M, Fernández-Iglesias A, Broqua P, Junien JL, Wettstein G, Bosch J, Gracia-Sancho J. Pan-PPAR agonist lanifibranor improves portal hypertension and hepatic fibrosis in experimental advanced chronic liver disease. J Hepatol. 2021 May;74(5):1188-1199. doi: 10.1016/j.jhep.2020.11.045. Epub 2020 Dec 2. PMID: 33278455. 3. Wettstein G, Luccarini JM, Poekes L, Faye P, Kupkowski F, Adarbes V, Defrêne E, Estivalet C, Gawronski X, Jantzen I, Philippot A, Tessier J, Tuyaa-Boustugue P, Oakley F, Mann DA, Leclercq I, Francque S, Konstantinova I, Broqua P, Junien JL. The new-generation pan-peroxisome proliferator-activated receptor agonist IVA337 protects the liver from metabolic disorders and fibrosis. Hepatol Commun. 2017 Jun 19;1(6):524-537. doi: 10.1002/hep4.1057. PMID: 29404476; PMCID: PMC5678909. 4. Ruzehaji N, Frantz C, Ponsoye M, Avouac J, Pezet S, Guilbert T, Luccarini JM, Broqua P, Junien JL, Allanore Y. Pan PPAR agonist IVA337 is effective in prevention and treatment of experimental skin fibrosis. Ann Rheum Dis. 2016 Dec;75(12):2175-2183. doi: 10.1136/annrheumdis-2015-208029. Epub 2016 Mar 9. PMID: 26961294; PMCID: PMC5136696.

In vitro protocol:

In vivo protocol:

1. Wettstein G, Luccarini JM, Poekes L, Faye P, Kupkowski F, Adarbes V, Defrêne E, Estivalet C, Gawronski X, Jantzen I, Philippot A, Tessier J, Tuyaa-Boustugue P, Oakley F, Mann DA, Leclercq I, Francque S, Konstantinova I, Broqua P, Junien JL. The new-generation pan-peroxisome proliferator-activated receptor agonist IVA337 protects the liver from metabolic disorders and fibrosis. Hepatol Commun. 2017 Jun 19;1(6):524-537. doi: 10.1002/hep4.1057. PMID: 29404476; PMCID: PMC5678909. 2. Ruzehaji N, Frantz C, Ponsoye M, Avouac J, Pezet S, Guilbert T, Luccarini JM, Broqua P, Junien JL, Allanore Y. Pan PPAR agonist IVA337 is effective in prevention and treatment of experimental skin fibrosis. Ann Rheum Dis. 2016 Dec;75(12):2175-2183. doi: 10.1136/annrheumdis-2015-208029. Epub 2016 Mar 9. PMID: 26961294; PMCID: PMC5136696.

1: Bruni C, Praino E, Allanore Y, Distler O, Gabrielli A, Iannone F, Matucci-Cerinic M. Use of biologics and other novel therapies for the treatment of systemic sclerosis. Expert Rev Clin Immunol. 2016 Dec 12:1-14. [Epub ahead of print] PubMed PMID: 27899043.