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Ravuconazole (BMS-207147) Sale

(Synonyms: 雷夫康唑; BMS-207147; ER-30346) 目录号 : GC32116

A triazole antifungal

Ravuconazole (BMS-207147) Chemical Structure

Cas No.:182760-06-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥462.00
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2mg
¥280.00
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5mg
¥420.00
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10mg
¥630.00
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25mg
¥1,540.00
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50mg
¥2,380.00
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Sample solution is provided at 25 µL, 10mM.

Description

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)

实验参考方法

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.
[2]. Fung-Tomc JC, et al. In vitro activity of a new oral triazole, BMS-207147 (ER-30346)Antimicrob Agents Chemother. 1998 Feb;42(2):313-8.
[3]. Hata K, et al. Efficacy of ER-30346, a novel oral triazole antifungal agent, in experimental models of aspergillosis, candidiasis, and cryptococcosis.Antimicrob Agents Chemother. 1996 Oct;40(10):2243-7.

化学性质

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
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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。
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溶解性数据

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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
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