Pirfenidone (S-7701) - Moligand™, 10mM in DMSO , CAS No.53179-13-8

CAS: 53179-13-8 Cat. No.: P409216 Molecular Weight: 185.22 Beilstein Registry Number: 21(5)7,197 EC Number: 621-260-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

AMR-69 | 2(1H)-Pyridinone, 5-methyl-1-phenyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Pirfenidone (S-7701, AMR-69) is an inhibitor forTGF-βproduction and TGF-β stimulated collagen production, reduces production ofTNF-αand IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuateschemokine (CC motif) ligand-2
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). 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.

In vivo

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. 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. 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. 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.
Cell Data

cell lines：Melanoma cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

AMR-69 | 2(1H)-Pyridinone, 5-methyl-1-phenyl-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Pirfenidone (S-7701, AMR-69) 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. Pirfenidone attenuates chemokine (CC motif) lig

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Product Properties

• ALogP: 1.9

Names and Identifiers

• Isomeric SMILES: CC1=CN(C(=O)C=C1)C2=CC=CC=C2
• WGK Germany: 3
• RTECS: UV1148200
• Molecular Weight: 185.22
• Beilstein: 21(5)7,197
• Reaxy-Rn: 1526549
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=1526549&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 48 mg/mL (200.63 mM); Ethanol: 3 mg/mL (12.53 mM); Water: Insoluble
• Melt Point(°C): 107.0 to 111.0 °C

References

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