Pirfenidone

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

Animal Study: ^[3]

References

貨號 Cat. No.: S2907
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Pirfenidone

Catalog No.S2907

Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 113	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 88	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Animal Models	Sprague-Dawley rats receiving a low-salt diet
Dosages	250 mg/kg
Administration	oral diet
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01136174	Completed	Idiopathic Pulmonary Fibrosis	Boehringer Ingelheim Pharmaceuticals	2010-05	Phase 2
NCT01366209	Active, not recruiting	Idiopathic Pulmonary Fibrosis	InterMune	2011-06	Phase 3
NCT01417156	Active, not recruiting	Pulmonary Fibrosis	Boehringer Ingelheim Pharmaceuticals	2011-09	Phase 2
NCT01504334	Recruiting	Idiopathic Pulmonary Fibrosis	Beijing Kawin Technology Share-Holding Co., Ltd.	2012-01	Phase 2
NCT01695408	Recruiting	Idiopathic Pulmonary Fibrosis	Dresden University of Technology\|GWT-TUD GmbH\|Boehringer Ingelheim Pharmaceuticals	2012-10

Description

Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.

In vitro

Pirfenidone (< 300 μg/mL) suppresses the proinflammatory cytokine tumor necrosis factor-α (TNF-α) by a translational mechanism in RAW264.7 cells, which is independent of activation of the mitogen-activated protain kinase (MAPK) 2, p38 MAP kinase, and c-Jun N-terminal kinase (JNK). ^[1] Pirfenidone (< 10 mM) leads to reduced glioma cell density in concentration-dependent manner in LN-18, T98G, LNT-229 and LN-308 cell lines. Pirfenidone (< 5 mM) reduces TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (< 8.3 mM) inhibits the activity of recombinant furin and downregulates the expression of MMP-11 in a dose-dependent manner in LN-308 cells. ^[2]

Pirfenidone (250 mg/kg) potently inhibits the production of the proinflammatory cytokines, TNF-alpha, interferon-gamma, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10, in mice. ^[1] Pirfenidone (250 mg/kg/day) ameliorates cyclosporine-induced fibrosis by about 50% and decreases TGF-beta1 protein expression by 80% in Sprague-Dawley rats receiving a low-salt diet. ^[3] Pirfenidone (400 mg/kg/day) inhibits heat shock protein 47-positive cells and myofibroblasts, the principal cells responsible for the accumulation and deposition of extracellular matrix seen in pulmonary fibrosis in ICR mice intravenously injected with bleomycin. ^[4] Pirfenidone (0.5%, liquid diet) treatment reduces the degree of liver injury in rats, as determined by alanine aminotransferase values and necro-inflammatory score, which is associated with reduced hepatic stellate cells proliferation and collagen deposition. Pirfenidone (0.5%, liquid diet) administration downregulates dimethylnitrosamine induced transcripts levels of procollagen alpha1(I), TIMP-1 and MMP-2 by 50-60% in rats, and this is associated with a 70% reduction in collagen deposition. ^[5]

Download Pirfenidone SDF

Molecular Weight (MW)	185.22
Formula	C₁₂H₁₁NO
CAS No.	53179-13-8

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	37 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	37 mg/mL (199 mM)
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W,	30 mg/mL
* <1 mg/ml means slightly soluble or 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.