MBP146-78 - Parasite 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMBP146-78Cat. No.: HY-101525CAS No.: 188343-77-3分式: CHFN分量: 335.42作靶点: Parasite作通路: Anti-infection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 : 7.69 mg/mL (22.93 mM; Need ultrasonic)Mass

2、Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9813 mL 14.9067 mL 29.8134 mL5 mM 0.5963 mL 2.9813 mL 5.9627 mL10 mM 0.2981 mL 1.4907 mL 2.9813 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件，适当保存；以下溶剂前的百分

3、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: 0.77 mg/mL (2.30 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.77 mg/mL (2.30 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.77 mg/mL (2.30 mM); Clear soluti

4、on1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 MBP146-78有效的选择性的cGMP依赖的蛋激酶抑制剂。体外研究 MBP146-78 displays a dose-dependent inhibition of T. gondii tachyzoites replicating inside HFFs, with anIC50 of 210 nM. The suppression of lytic parasite growth by MBP146-78 is reversible. Re

5、placement of themedium with medium lacking MBP146-78, after treatment for up to 7 days at 2 M, results in complete lysisof HFF cell monolayers. MBP146-78 is neither toxic nor inhibitory to proliferating or confluent monolayers ofHFFs at concentrations of up to 10 M 1.体内研究 In infected mice that are t

6、reated with MBP146-78 at 50 mg/kg twice daily, parasites are undetectablethroughout the 10-day treatment period in each of the tissues examined. However, samples from brain,spleen, and lung taken from infected treated mice reveal the presence of parasites after cessation ofadministration of MBP146-7

7、8, indicating that a transient asymptomatic parasite recrudescence occurs in allsurvivors. The ability of mice to control Toxoplasma infection after MBP146-78 treatment has beenterminated suggests that the mouse immune system plays a synergistic role with chemotherapy in controllingthe infection 1.P

8、ROTOCOLCell Assay 1 To assess the toxicity of MBP146-78 to HFFs, cells are plated in 96-well plates at 1000/well and allowed toadhere overnight prior to addition of compound. Cultures are incubated for 5 days at 37C in the presence of5% CO2. Viability is assessed using the Cell-Titer 96 Aqueous One

9、solution cell-proliferating assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: MBP146-78 is dissolved in water. MBP146-78 is administered in 100 L doses by intraperitonealAdministration 1 injections starting 24 h after parasite inocula

10、tion. Mice are monitored twice daily for clinical evidence oftoxoplasmosis and mortality throughout the experimental period 1.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 Front Microbiol. 2018 Jun 12;9:1266.See more customer validations o

11、n HYPERLINK / www.MedChemEREFERENCES1. Nare B, et al. Evaluation of a cyclic GMP-dependent protein kinase inhibitor in treatment of murine toxoplasmosis: gamma interferon isrequired for efficacy. Antimicrob Agents Chemother. 2002 Feb;46(2):300-7.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not