MBP146-78 - Parasite 抑制劑 - 生命科學(xué)試劑 - 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作靶點(diǎn): Parasite作通路: Anti-infection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 : 7.69 mg/mL (22.93 mM; Need ultrasonic)Mass

2、Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)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(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)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?qǐng)先配制澄清的儲(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)存條件，適當(dāng)保存；以下溶劑前的百分

3、指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.77 mg/mL (2.30 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.77 mg/mL (2.30 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.77 mg/mL (2.30 mM); Clear soluti

4、on1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 MBP146-78有效的選擇性的cGMP依賴的蛋激酶抑制劑。體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師www.MedChemECaution: Product has not