AEBSF-hydrochloride _Thrombin 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAEBSF hydrochlorideCat. No.: HY-12821CAS No.: 30827-99-7分式: CHClFNOS分量: 239.69作靶点: Thrombin作通路: Metabolic Enzyme/Protease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 (417.21 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.1721 mL 20.8603 mL 41.7206 mL5 mM 0.8344 mL 4.1721 mL 8.3441 mL10 mM 0.4172 mL 2.0860 mL 4.1721 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

3、可以根据储存条件，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: 2.5 mg/mL (10.43 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.43 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (

4、10.43 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 AEBSF hydrochloride丝氨酸蛋酶 的不可逆抑制剂，可抑制例如胰凝乳蛋酶，激肽释放酶，纤溶酶，凝酶和胰蛋酶。体外研究 AEBSF inhibits the constitutive production of A by directly inhibiting -secretase in five different human celllines, both neural and nonn

5、eural 1. AEBSF, as a serine protease inhibitor, inhibits the lysis of leukemic cellsby human macrophages without inhibiting macrophage secretion of TNF- and IL-1 2. AEBSF alsodisturbs the growth of blastocysts on endometrial cells and inhibit the adhesion of HeLa cells on HUVECs byaltering the prote

6、in secretion pattern 4.体内研究 AEBSF (76.8 mg/kg daily, i.p.) results in prolongation of the survival of mice that have been given a lethal T.gondii infection 3. AEBSF also reduces airway response and underlying inflammation in cockroach allergen-induced murine model 4.PROTOCOLCell Assay 4 The HeLa cel

7、ls suspended in RPMI-1640 media containing 10% FCS are plated into each well of a 96-wellmicroplate (5103 cells/200 L/well). After incubation for 24 h at 37C, cells are treated with different dosesof AEBSF (0, 25, 50, 100 g/mL) for 48 h. Then, 20 L fresh 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-dipheny

8、tetrazoliumromide (MTT) reagent (5 g/L) is added into each well, and cells are cultured at 37C in5% CO2 for another 4 h. The media are discarded carefully, and 150 L DMSO is added. Absorbance is readon a microplate reader at dual wavelengths of 540 and 620 nm.MCE has not independently confirmed the

9、accuracy of these methods. They are for reference only.Animal Mice injected with 2.5103 parasites are randomLy assigned to one of the treatment groups according to theAdministration 3 treatment given: without drugs (control group), vehicle alone (vehicle control group), pyrimethamine alone atdiffere

10、nt doses, LY311727 alone at different doses, AEBSF alone at different doses or AEBSF 76.8 mg/kgplus pyrimethamine 10 mg/kg. Each treatment group consists of 10 animals. Treatment is initiated 24 h afterparasite inoculation and is continued for seven consecutive days. Mouse survival is monitored dail

11、y andcontinued in live mice until 15 days post-infection. All experiments are performed three times and the datashown represent the cumulative results.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Int J Oncol. 2019 May.See more customer va

12、lidations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Citron M, et al. Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF. Neuron. 1996Jul;17(1):171-92. Nakabo Y, et al. Lysis of leukemic cells by human ma

13、crophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), aserine protease inhibitor. J Leukoc Biol. 1996 Sep;60(3):328-36.3. Buitrago-Rey R, et al. Evaluation of two inhibitors of invasion: LY311727 3-(3-acetamide-1-benzyl-2-ethyl-indolyl-5-oxy)propanephosphonic acid and AEBSF 4-(

14、2-aminoethyl)-benzenesulphonyl fluoride in acute murine toxoplasmosis. J Antimicrob Chemother.4. Jiang YH, et al. Serine protease inhibitor 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF) inhibits the rat embryoimplantation in vivo and interferes with cell adhesion in vitro. Contraception. 2011 Dec;84(