Calpeptin - Cathepsin 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECalpeptinCat. No.: HY-100223CAS No.: 117591-20-5分式: CHNO分量: 362.46作靶點(diǎn): Cathepsin; Proteasome作通路: Metabolic Enzyme/Protease儲(chǔ)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 : 155 mg/mL (427.63 m

2、M)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.90 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.90 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Calpeptin種有效的、具有細(xì)胞穿透性的 calpain 抑制劑，其對(duì)板 Calpain I 的ID50 值為4

3、0 nM 1。Calpeptin 也是cathepsin K 的抑制劑 2。IC50 & Target ID50: 40 nM (Calpain I in human platelets) 1.Cthepsin K 2體外研究 Calpeptin (0-100 nM, 24 hours) treatment suppresses the proliferation of both WI38 VA13 and IMR90 cells ina dose-dependent manner. Calpeptin (1000 pg/ml, 24 hours) inhibits IL-6-induced

4、cell proliferation of lungfibroblasts 3.Cell Proliferation Assay 3Cell Line: WI38 VA13 and IMR90 cellsConcentration: 0-100 nMIncubation Time: 24 hoursResult: Suppressed the proliferation in a dose-dependent manner.體內(nèi)研究 Calpeptin with Bleo (0.04 mg/mouse, i.p., 3 times weekly, 28 days) administration

5、 significantly inhibits thecollagen deposition and increases of calpain activity in the bleomycin treated mouse lung tissues 3.Animal Model: C57BL/6 female mice (Eight-week-old) 3.Dosage: 0.04 mg/mouse.Administration: Intraperitoneally three times weekly for 28 days (together with Bleo).Result: Inhi

6、bited the collagen deposition and increase of calpain activity in the bleomycintreatedmouse lung tissues.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) RSC Adv. 2019 Aug.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem

7、Biophys Res Commun. 1988 Jun30;153(3):1201-8.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22.3. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc