Ravuconazole (BMS-207147)
(Synonyms: 雷夫康唑; BMS-207147; ER-30346) 目录号 : GC32116
A triazole antifungal
Cas No.:182760-06-1
Sample solution is provided at 25 µL, 10mM.
Ravuconazole is an orally available triazole fungicide that potently inhibits the growth of a wide range of fungi (MICs range from 25 to 780 ng/ml).1,2 Like other azoles, ravuconazole inhibits cytochrome P450 (CYP) isoforms that are involved in ergosterol biosynthesis, interfering with the generation of the fungal and protozoan cell membranes.3 Ravuconazole specifically inhibits sterol 14α-demethylase (CYP51).4,5 As this enzyme is also important in the development of trypanosomes, ravuconazole is effective against T. cruzi infections in animal models of Chagas disease.4,5
1.Hata, K., Kimura, J., Miki, H., et al.In vitro and in vivo antifungal activities of ER-30346, a novel oral triazole with a broad antifungal spectrumAntimicrob. Agents Chemother.40(10)2237-2242(1996) 2.Hata, K., Kimura, J., Miki, H., et al.Efficacy of ER-30346, a novel oral triazole antifungal agent, in experimental models of aspergillosis, candidiasis, and cryptococcosisAntimicrob. Agents Chemother.40(10)2243-2247(1996) 3.Carillo-Mu?oz, A.J., Giusiano, G., Ezkurra, P.A., et al.Antifungal agents: mode of action in yeast cellsRev.Esp.Quimioter.19(2)130-139(2006) 4.Urbina, J.A., Payares, G., Sanoja, C., et al.In vitro and in vivo activities of ravuconazole on Trypanosoma cruzi, the causative agent of Chagas diseaseInt.J.Antimicrob.Agents21(1)27-38(2003) 5.Lepsheva, G.I.Design or screening of drugs for the treatment of Chagas disease: What shows the most promise?Expert Opin.Drug Discov.8(12)1479-1489(2013)
Animal experiment: | Mouse[1] Ravuconazole is prepared in 10% DMSO in 0.5% CMC.C. neoformans No. 3 is grown on an SDA plate at 30°Cfor 48 h, and challenge organisms are prepared in sterile saline. Mice (age, 5 weeks; n 5 10) are infected via the tail vein. Ravuconazole are orally administered, in a volume of 0.2 mL per dose, twice daily for 5 consecutive days starting 1 h after infection. Controls receive 10% DMSO in 0.5% CMC. Ravuconazole are administered at doses of 8 and 32 mg/kg. Mortality is recorded daily for 21 days of infection. Drug efficacy is assessed by determining the delay in mortality. Rats[3] The rats are orally infected three times at 48-h intervals with 0.1 mL of a saline suspension containing cells of C. albicansE81022. Ravuconazoleis orally administered, in a volume of 0.5 mL per dose, once daily for 3 consecutive days starting 2 days after the last infection. Control groups receive 10% DMSO in 0.5% CMC. Drugs are administered at doses of 1 and 4 mg/kg. Drug efficacy is assessed 5 days after the last infection by measuring the number of C. albicansorganisms in oral swabs. |
References: [1]. Hata K, et al. In vitro and in vivo antifungal activities of ER-30346, a novel oral triazole with a broad antifungal spectrum.Antimicrob Agents Chemother. 1996 Oct;40(10):2237-42. |
Cas No. | 182760-06-1 | SDF | |
别名 | 雷夫康唑; BMS-207147; ER-30346 | ||
Canonical SMILES | FC1=CC(F)=CC=C1[C@](CN2C=NC=N2)(O)[C@@H](C)C3=NC(C4=CC=C(C#N)C=C4)=CS3 | ||
分子式 | C22H17F2N5OS | 分子量 | 437.47 |
溶解度 | DMSO : ≥ 50 mg/mL (114.29 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
General tips | 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.2859 mL | 11.4294 mL | 22.8587 mL |
5 mM | 0.4572 mL | 2.2859 mL | 4.5717 mL |
10 mM | 0.2286 mL | 1.1429 mL | 2.2859 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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