Buparvaquone - Parasite 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBuparvaquoneCat. No.: HY-17581CAS No.: 88426-33-9分式: CHO分量: 326.43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 : 33.33 mg/mL (102.10 mM; Need ultrasonic)Mas

2、s Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0634 mL 15.3172 mL 30.6344 mL5 mM 0.6127 mL 3.0634 mL 6.1269 mL10 mM 0.3063 mL 1.5317 mL 3.0634 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

3、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 (7.66 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.66 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.

4、66 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Buparvaquone种与parvaquone和atovaquone有关的羟 萘醌类抗原药。体外研究 In 4-day proliferation assays, buparvaquone efficiently inhibits N.caninum tachyzoite replication(IC50=4.9nM; IC100=100nM) 1. Buparvaquone is significantl

5、y selective against L. (L.) infantum chagasi intracellularamastigotes, with an IC50 value of 1.5 M. Other cutaneous species are also susceptible to buparvaquone,with IC50 values in the range 1-4 M 2.体内研究 Treatment of N.caninum infected mice with buparvaquone (100mg/kg) either by intraperitoneal inje

6、ction orgavage prevents neosporosis symptoms in 4 out of 6 mice in the intraperitoneally treated group, and in 6 outof 7 mice in the group receiving oral treatment 1. Both a hydrous gel and water-in-oil emulsion ofbuparvaquone significantly reduce cutaneous parasite burden and lesion size, compared

7、with the untreatedcontrol 3.PROTOCOLCell Assay 1 To study whether pretreatment of host cells prior to invasion had any effect on parasite proliferation,confluent HFF grown in 6-well plates are treated with 1M buparvaquone in medium for 1h or 5h, andcontrols are exposed to the corresponding amounts o

8、f DMSO. Subsequently, the drug-containing medium isremoved and monolayers are ished 4 times with Hanks Balanced Salt Solution, and are infected with Nc-Livtachyzoites in 5mL medium without any drug or solvent. After 2 days, cells are collected with a cell scraper,centrifuged, ished once more in PBS,

9、 and the pellet is stored at 20C prior to quantification of N.caninumproliferation by N.caninum-specific real time PCR as outlined below 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: On day 0, all mice are infected by intraperitoneal (i

10、.p.) injection of freshly purified N.caninumAdministration 1 tachyzoites. After 48h, mice receive BPQ (100mg/kg) as suspension in corn oil either by i.p. injection of avolume of 100l or by oral application of 100l by gavage. The control groups obtained the correspondingamount of the solvent only, ei

11、ther i.p. or orally (see Table 2). The treatments are performed 5 times on a dailybasis. If not indicated otherwise, mice are inspected twice daily for clinical signs (ruffled coat, apathy, hindlimb paralysis) until day 21 post infection (p.i.), at which time they are euthanized 1.MCE has not indepe

12、ndently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mller J, et al. Buparvaquone is active against Neospora caninum in vitro and in experimentally infected mice. Int J Parasitol Drugs DrugResist. 2015 Feb 13;5(1):16-25.2. Reim?o JQ, et al. Effectiveness of lipos

13、omal buparvaquone in an experimental hamster model of Leishmania (L.) infantum chagasi. ExpParasitol. 2012 Mar;130(3):195-9.3. Garnier T, et al. In vivo studies on the antileishmanial activity of buparvaquone and its prodrugs. J Antimicrob Chemother. 2007Oct;60(4):802-10.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdf