|rel-1-(4-(((2R,4S)-2-((1H-1,2,4-三唑-1-基)甲基)-2-(2,4-二氯苯基)-1,3-二氧杂环戊烷- 4-基)甲氧基)苯基)-4-异丙基哌嗪|CsnPharm

CAS No.: 67915-31-5

特康唑 Catalog No. CSN12055

Synonyms: R42470;NSC 331942;R-42,470

Terconazole is used to treat vaginal yeast infection, working by disrupting the biosynthesis of fats in a yeast cell.

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技术信息

生物活性

描述Terconazole is a new broad-spectrum antifungal agent for the treatment of vulvovaginal candidiasis. In US studies of 80-mg terconazole suppositories, clinical cure rates 8 to 10 days after therapy were between 89% and 92%, and microbiologic cure rates were between 80% and 85%^[3]. Terconazole has far greater selectively for yeast cytochrome P-450 than for mammalian microsomal cytochrome P-450. The spectrum of terconazole's in vitro activity includes a wide range of pathogenic fungi; in Eagle's Minimum Essential Medium, fungicidal activity against all strains of Candida albicans occurred at less than or equal to 100 ng/mL^[4]. Terconazole blocked the morphogenetic transformation from the yeast into the filamentous form at concentrations of 0.008 to 0.05 mg/mL. In experimental candidiasis in castrated rats with estrogen-induced permanent pseudoestrus, topical treatment with terconazole was superior to miconazole, clotrimazole, econazole, butoconazole, tioconazole, sulconazole, bifonazole, valconazole, fenticonazole, nystatin, and amphotericin B in the various schedules used. A 3-day once-daily intravaginal application of terconazole 0.8% was usually sufficient to provide a functional therapeutic period of 7 days because of prolonged high biologically active antifungal levels in the vagina. No side effects were observed at any concentration of terconazole^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00503542	Vaginitis	Early Phase 1	Completed	-	United States, New York ... more >> Family Health Center Bronx, New York, United States, 10458 Collapse <<
NCT01813162	HIV Prevention	Phase 1	Completed	-	United States, California ... more >> Dept of OBGYN and Reproductive Sciences, UCSF San Francisco, California, United States United States, New York Bronx-Lebanon Hospital Center Bronx, New York, United States Collapse <<
NCT02308007	Vaginal Infection	Phase 3	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8781 mL
- 9.3903 mL
- 18.7807 mL
- 5 mM
- 0.3756 mL
- 1.8781 mL
- 3.7561 mL
- 10 mM
- 0.1878 mL
- 0.9390 mL
- 1.8781 mL

技术信息

CAS号

67915-31-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H31Cl2N5O3

运输

蓝冰

分子量

532.46

别名

R42470;NSC 331942;R-42,470;Gyno-Terazol;Terconazolum;特康唑

溶解度

DMSO	47.0 mg/mL (88.3 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (187.8 mM)

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