Bufalin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBufalinCat. No.: HY-N0877CAS No.: 465-21-4分式: CHO分量: 386.52作靶点: Na+/K+ ATPase作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (258.72 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5872 mL 12.9359 mL 25.8719 mL5 mM 0.5174 mL 2.5872 mL 5.1744 mL10 mM 0.2587 mL 1.2936 mL 2.5872 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条

3、件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.38 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.38 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.38 m

4、M); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Bufalin是蟾酥中的有效活性成分，为有效的 Na+/K+-ATPase 抑制剂，可与其基1, 2 和 3 结合，Kd 值分别为 42.5，45 和 40 nM 1 2。具有抗肿瘤活性 2。IC50 & Target Kd: 42.5 nM (Na,K-ATPase 1), 45 nM (Na,K-ATPase 2), 40 nM (Na,K-ATPase 3) 1体外研究 Bufalin (0, 1, 2, 4

5、M for 48 hours) decreases cell viability in NCI-H460 cells 2.Bufalin (2 M) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78mRNA expression 2.Cell Viability Assay 2Cell Line: NCI-H460 cellsConcentration: 0, 1, 2, 4 MIncubation Time: 48 hoursResult: Decreased viability o

6、f NCI-H460 cells in a dose-dependent manner.体内研究 Bufalin (0.1, 0.2, or 0.4 mg/kg, i.p., daily for 14 days) shows significant anti-tumor activity in mice bearingNCI-H460 cells 2.Animal Model: Forty male athymic BALB/c nu/nu mice (6-8 weeks old) 2Dosage: 0.1, 0.2, or 0.4 mg/kgAdministration: I.P. ever

7、y day until 14 daysResult: Dose-dependently suppressed tumor growth.REFERENCES1. Katz A, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010 Jun 18;285(25):19582-92.2. Wu SH, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. EnvironToxicol. 2017 Apr;32(4):1305-1317.McePdfHeightCaution: Product has not been fully validated for medical applications.For resear