1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETargocilCat. No.: HY-18702CAS No.: 1200443-21-5分式: CHClNOS分量: 475.95作靶點: Bacterial作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 33.33 mg/mL (70.03 mM; Need ultrasonic)H

2、2O : 90% corn oilSolubility: 2.5 mg/mL (5.25 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Targocil 可作磷壁酸 (WTA) 物合成的抑抑制劑，可抑制甲氧西林敏感 葡萄球菌(MSSA）和耐甲氧西林 葡萄球 (MRSA) 的長，對于 MRSA 和 MSSA 的 MIC90 值都為 2 g/mL。IC50 & Target MIC90: 2 g/mL (MSSA), 2 g/mL (MRSA) 1體外研究 MIC

3、s of Targocil against S. aureus strains Newman, MW2, MG2375, and MG2389 are 1 g/mL for all strains.Targocil shows excellent activity against S. aureus isolates from suspected cases of bacterial keratitis,including both MSSA and MRSA isolates, with MICs that range from 1 to 2 g/ mL. Targocil, a deriv

4、ative of1835F03, exhibits better activity against all keratitis isolates than the original lead compound, 1835F03. Bovineserum exhibits a detectable but moderate inhibitory effect on the in vitro antimicrobial activities of both1835F03 and Targocil, increasing the MICs of both by 4- to 8-fold. Compa

5、re to the vehicle alone, Targocil at 5g/mL exhibits little toxicity for HCECs, even after 24 h of exposure. However, 40 g/mL Targocil showstoxicity at all time points tested. Targocil at levels equal to 10MIC in vitro readily inhibits growth of Newmanand MG2375 in the presence of HCECs 1PROTOCOLCell

6、 Assay 1 Log-phase strains MG2375, MG2389, Newman, and MW2 are collected and adjusted to a concentration of2108 CFU/mL. After the treatment of bacterial cultures with Targocil at 10MIC for 1 h, the cells are diluted1:1,000 in fresh medium and then incubated and plated at the appropriate time points

7、for viabilitydetermination. The postantibiotic effect (PAE) is calculated by the standard equation T-C, where T is the timerequired for the CFU count in the test culture to increase 10-fold above the count observed immediately afterdrug removal, and C is the time required for the count of the untrea

8、ted control to increase 10-fold under thesame conditions 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Suzuki T, et al. In vitro antimicrobial activity of wall teichoic acid biosynthesis inhibitors against Staphylococcus aureus isolates.Antimicrob Agents Chemother. 2011 Feb;55(2):767-74.McePdfHeightCaution: Product has not been fully validated for medical applicati