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CAS No.: 927961-18-0

Lanifibranor Catalog No. CSN20539

Synonyms: IVA337

IVA-337 is a agonist of peroxisome proliferator-activated receptors (PPAR) which is widely used in the study of lung fibrosis and pulmonary hypertension.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述IVA337 is a moderately potent and well balanced pan PPAR agonist with ECC50 values of 1.54μM, 0.866μM and 0.206μM for hPPARα, hPPARδ and hPPARγ, respectively. IVA337 demonstrated significant activation of PPARα and PPARδ as it increased beta-oxidation by 44%, 79% and 113% in HuH7 cells at 1μM, 3μM and 10μM, respectively, and 12%, 37%, 67% and 55% in C2C12 cells at 1μM, 3μM, 10μM and 30μM, respectively. It induced gene expression of aP2 by 6%, 18%, 47%, 78%, 97% and 70%, and gene expression of Adiponectine by 7%, 16%, 42%, 62%, 80% and 56% at concentration of 0.1μM, 0.3μM, 1μM, 3μM, 10μM and 30μM. IVA337 reduced plasma glucose by 40% at 10mg/kg and 58% at 30 mg/kg, as well as reduced triglycerides by 33% at 10mg/kg and 45% at 30mg/kg in db/db mice. Oral administration of IVA337 once a day significantly reduced collagen deposition and increased adiponectin at 30mg/kg in CCl4-induced liver fibrosis in mice after 3 weeks of treatment^[3].
作用机制IVA337 adopts a T-shape conformation and filling an additional sub-pocket with specific hydrogen bond interactions between its carboxylic acid and both E343 and R288 of PPARγ.^[3]

动物研究

剂量

Mice: 30 mg/kg - 100 mg/kg^[2] (p.o.), 10 mg/kg - 30 mg/kg^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[1]
Dose	10 mg/kg
Administration	p.o.
C_max	10710 ng/ml
T_max	1 h
AUC_inf	29367 h·(ng/ml)

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03459079	Nonalcoholic Fatty Liver Disea... more >>se (NAFLD) Type 2 Diabetes (T2DM) Collapse <<	Phase 2	Recruiting	March 2020	United States, Florida ... more >> University of Florida Recruiting Gainesville, Florida, United States, 32610 Contact: Danielle Poulton 352-294-4895 Danielle.Poulton@medicine.ufl.edu Contact: Amanda Slater 352-294-4896 amanda.slater@medicine.ufl.edu Sub-Investigator: Fernando Bril, MD Sub-Investigator: Diana Barb, MD Sub-Investigator: Troy Donahoo, MD Sub-Investigator: Julio Leey, MD Collapse <<
NCT03008070	Non-Alcoholic Steatohepatitis ... more >>(NASH) Collapse <<	Phase 2	Recruiting	January 2020	-
NCT02503644	Scleroderma, Diffuse ... more >> Diffuse Cutaneous Systemic Sclerosis Collapse <<	Phase 2	Active, not recruiting	November 2018	-

参考文献

[1] Boubia B, Poupardin O, et al. Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate. J Med Chem. 2018 Mar 22;61(6):2246-2265.
[2] Avouac J, Konstantinova I, et al. Pan-PPAR agonist IVA337 is effective in experimental lung fibrosis and pulmonary hypertension. Ann Rheum Dis. 2017 Nov;76(11):1931-1940.
[3] Boubia B, Poupardin O, Barth M, Binet J, Peralba P, Mounier L, Jacquier E, Gauthier E, Lepais V, Chatar M, Ferry S, Thourigny A, Guillier F, Llacer J, Amaudrut J, Dodey P, Lacombe O, Masson P, Montalbetti C, Wettstein G, Luccarini JM, Legendre C, Junien JL, Broqua P. Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate. J Med Chem. 2018 Mar 22;61(6):2246-2265. doi: 10.1021/acs.jmedchem.7b01285. Epub 2018 Feb 27. PMID: 29446942.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2993 mL
- 11.4965 mL
- 22.9929 mL
- 5 mM
- 0.4599 mL
- 2.2993 mL
- 4.5986 mL
- 10 mM
- 0.2299 mL
- 1.1496 mL
- 2.2993 mL

技术信息

CAS号

927961-18-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15ClN2O4S2

运输

蓝冰

分子量

434.92

别名

IVA337

溶解度

DMSO	84.0 mg/mL (193.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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