Pirfenidone-AMR69-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPirfenidoneCat. No.: HY-B0673CAS No.: 53179-13-8Synonyms: AMR69分式: CHNO分量: 185.22作靶點(diǎn): TGF-beta/Smad作通路: Stem Cell/Wnt; TGF-beta/Smad儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL

2、 (539.90 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 5.3990 mL 26.9949 mL 53.9898 mL5 mM 1.0798 mL 5.3990 mL 10.7980 mL10 mM 0.5399 mL 2.6995 mL 5.3990 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實(shí)

3、驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (13.50 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (13.50 mM); Clear solution1/3 Master of Small Molecu

4、les 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (13.50 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pirfenidone種于治療特發(fā)性肺纖維化的藥物。 它抑制FGFR，EGFR，PDGFR，TGF-，從減緩腫瘤細(xì)胞增殖。IC50 & Target TGF-2 1體外研究 Pirfenidone (PFD) reduces the protein levels of the matrix metalloproteinase (MMP)-1

5、1, a TGF- target geneand furin substrate involved in carcinogenesis. These data define PFD or PFD-related agents as promisingagents for human cancers associated with enhanced TGF- activity 1. In RAW264.7 cells, a murinemacrophage-like cell line, Pirfenidone suppresses the proinflammatory cytokine TN

6、F- by a translationalmechanism, which is independent of activation of the MAPK2, p38 MAPK, and JNK. In the murine endotoxinshock model, Pirfenidone potently inhibits the production of the proinflammatory cytokines, TNF-, interferon-, and interleukin-6, but enhances the production of the anti-inflamm

7、atory cytokine, interleukin-10 2.Pirfenidone (PFD) shows its inhibitory effects on the proliferation of HLECs. Cell proliferation is attenuated inthe 0.3 mg/mL group after 24 hours compare with the control group (P=0.044). The effect is more apparent inthe 0.5 mg/mL group at 24, 48, and 72 hours (P

8、3.體內(nèi)研究 Administration of Pirfenidone (300 mg/kg/day) for 4 wk. Pirfenidone significantly attenuates the score whenadministered in Bleomycin (BLM)-treated mice (P 4.PROTOCOLCell Assay 3 HLECs are seeded in 96-well plates (1104 cells/well) for 24 hours in -MEM/10% FBS/1%NEAA, and arecultured in statio

9、nary tubes in serum-free medium for 24 hours. And then the culture medium is removed andcells are bathed in -MEM with 10% FBS and 1% NEAA supplemented with 0, 0.01, 0.1, 0.2, 0.3, 0.5, or 1mg/mL Pirfenidone for 0, 4, 12, 24, 48, or 72 hours. After incubation with 180 L -MEM and 20 L of 5mg/mL MTT fo

10、r 4 hours at 37C, the MTT solution is discarded. The Formosan precipitates are dissolved in180 L DMSO by agitating the dishes for 10 minutes at 200 rpm on an orbital shaker. The absorbance at 490nm in each well is read with a micro plate reader. We further examined the effects of PFD by refining the

11、concentrations at 0.2, 0.25, 0.3, 0.4, 0.5 and 0.6 mg/mL using the MTT assay 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 4Administration 4 Nine-week-old female C57BL/6 mice are used. Pirfenidone is administered orally for 14 days after

12、 osmoticpump implantation. The volume of administration is determined according to body weight. Animals areallocated into 4 groups (n=6/group): normal control, BLM, Pirfenidone (300 mg/kg/day), and BLM +Pirfenidone. The Pirfenidone dose is selected according to a report published elsewhere. Pirfenid

13、one is alsoadministered in a therapeutic setting beginning at day 10 to assess the effect of the drug on the fibrotic phase2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEof BLM model mice.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J E

14、thnopharmacol. 2019 Apr 12:111878. Radiat Res. 2018 Oct;190(4):396-403. Pathol Res Pract. 2019 Jul. Oncotarget. 2018 May 4;9(34):23462-23481.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Burghardt I, et al. Pirfenidone inhibits TGF-beta expression in malignant glioma cells. B

15、iochem Biophys Res Commun. 2007 Mar9;354(2):542-7.2. Nakazato H, et al. A novel anti-fibrotic agent pirfenidone suppresses tumor necrosis factor-alpha at the translational level. Eur JPharmacol. 2002 Jun 20;446(1-3):177-85.3. Yang Y, et al. Inhibition of Pirfenidone on TGF-beta2 induced proliferatio

16、n, migration and epithlial-mesenchymal transitionof human lensepithelial cells line SRA01/04. PLoS One. 2013;8(2):e56837.4. Inomata M, et al. Pirfenidone inhibits fibrocyte accumulation in the lungs in bleomycin-induced murine pulmonary fibrosis. Respir Res.2014 Feb 8;15:16.5. Brooks D, et al. Limited fibrosis accompanies triple-negative breast cancer metastasis in multiple model systems and is not a preventivetar