Bufalin-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBufalinCat. No.: HY-N0877CAS No.: 465-21-4分式: CHO分量: 386.52作靶點(diǎn): Na+/K+ ATPase作通路: Membrane Transporter/Ion Channel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 : 100 mg/mL (258.72 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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(chǔ)備液，并請注意儲(chǔ)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(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的?chǔ)備液，再依次添加助溶劑(為保證實(shí)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；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條

3、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: 2.08 mg/mL (5.38 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.38 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.38 m

4、M); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Bufalin是蟾酥中的有效活性成分，為有效的 Na+/K+-ATPase 抑制劑，可與其基1, 2 和 3 結(jié)合，Kd 值分別為 42.5，45 和 40 nM 1 2。具有抗腫瘤活性 2。IC50 & Target Kd: 42.5 nM (Na,K-ATPase 1), 45 nM (Na,K-ATPase 2), 40 nM (Na,K-ATPase 3) 1體外研究 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.體內(nèi)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