Robenidine-hydrochloride _Bacterial 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERobenidine hydrochlorideCat. No.: HY-B2157CAS No.: 25875-50-7分式: CHClN分量: 370.66作靶點(diǎn): Bacterial; 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 : 30 mg/mL (80.94 mM

2、)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.6979 mL 13.4895 mL 26.9789 mL5 mM 0.5396 mL 2.6979 mL 5.3958 mL10 mM 0.2698 mL 1.3489 mL 2.6979 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。BIOLOGICAL ACTIVITY物活性 Robenidine hydrochloride種抗球藥, 對(duì) MRSA 和 VR

3、E 也有抑制活性，其 MIC50 值分別為 8.1 和 4.7 M。IC50 & Target MIC50: 8.1 M (MRSA), 4.7 M (VRE) 1體外研究Robenidine (compound 1) inhibits the growth of MRSA and VRE with MIC values of 8.1 and 4.7 M,1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemErespectively. Robenidine is bactericidal against all of the S. aureus st

4、rains tested with MBC/MIC90 ratios 2.A profound and negative impact on the MIC values with a 4-fold decrease with Robenidine at 2% serum andno activity at 50% serum is observed 1.體內(nèi)研究 The time that the mean plasma concentration exceeds the concentration of 1 g/mL is approximately 6 h inthe Florfenic

5、ol (FFC) alone group; however, it is lowered to 4 h by Robenidine (ROB) pretreatment. Theterminal elimination half-life (t1/2z), area under the concentration-time curve (AUC), area under the firstmoment curve (AUMC), and mean residence time (MRT) significantly decreased, whereas the eliminationrate

6、constant (z) and total body clearance (CLz) obviously increased in rabbits pretreated with Robenidine2.PROTOCOLCell Assay 1 MRSA clinical isolates are used in this study and the MIC50 for Robenidine (compound 1) is determinedusing a modified MIC assay. The antimicrobial dilutions of Robenidine are c

7、ompleted in 100% DMSO, with 2L added to each well. The assay is performed in a total volume of 200 L in 96-well plates. Robenidine istested in final concentrations of 0.7 to 345.3 M. Plates are incubated for 20 to 24 h at 37C beforedetermination of the MIC 1.MCE has not independently confirmed the a

8、ccuracy of these methods. They are for reference only.Animal The rabbits are divided into four groups (n=8, each group). The rabbits in the control group are fedAdministration 2 anticoccidial-free rations throughout the study. Rabbits in the other group are fed rations containingRobenidine (ROB) (66

9、 ppm) for 20 consecutive days. At the end of the 20th day of feeding, a single dose ofFlorfenicol (FFC) is injected intravenously at 25 mg/kg body weight (b.w.) into the left auricular vein of eachrabbit in all groups. Blood (approximately 1 mL) samples are collected into heparin-coated tubes from t

10、heright auricular vein of each rabbit at 5, 10, 15, 30, and 45 min and 1, 1.5, 2, 4, 6, 8, and 12 h afteradministration of FFC. The plasma is harvested after centrifugation at 3,000 g for 10 min and stored at -20Cuntil analysis 2.MCE has not independently confirmed the accuracy of these methods. The

11、y are for reference only.REFERENCES1. Abraham RJ, et al. Robenidine Analogues as Gram-Positive Antibacterial Agents. J Med Chem. 2016 Mar 10;59(5):2126-38.2. Liu C, et al. Influence of three coccidiostats on the pharmacokinetics of florfenicol in rabbits. Exp Anim. 2015;64(1):73-9.McePdfHeightCaution: Product has not b