Terconazole (R42470)
(Synonyms: 特康唑; R42470) 目录号 : GC32131
A triazole antifungal
Cas No.:67915-31-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: The rats are infected intravaginally with C. albicans. They are treated topically twice daily for 3 days, starting 24 hours after infection with a volume of 0.2 mL of various concentrations of terconazole (0.125%, 0.25%, 0.4%, 0.5%, 1%, 2%), miconazole, clotrimazole, econazole, nystatin, or amphotericin B[2]. |
References: [1]. Tolman EL, et al. Anticandidal activities of terconazole, a broad-spectrum antimycotic. Antimicrob Agents Chemother. 1986 Jun;29(6):986-91. | |
Terconazole is an orally bioavailable broad-spectrum triazole antifungal agent that completely inhibits growth of T. rubrum, M. audouini, M. canis, and T. verrucosum, as well as some C. albicans and A. fumigatus strains and other fungi when used at a concentration of 100 μg/ml.1 It also has bacteriostatic activity against E. coli, P. aeruginosa, S. aureus, and S. pyogenes when used at a concentration of 100 μg/ml. Terconazole eliminates vaginal C. albicans candidiasis infection in 97% of rats when administered as a 1% topical ointment and in 50% of rats when orally administered at a dose of 10 mg/kg. It inhibits cytochrome P450 (CYP) isoforms involved in ergosterol biosynthesis, interfering with fungal cell membranes.2 It decreases synthesis of 14α-desmethyl sterols and increases synthesis of methylated sterols in C. albicans (IC50 = 3 nM).3 Formulations containing terconazole have been used in the treatment of candidiasis of the vulva and vagina.
1.Van Cutsem, J., Van Gerven, F., Zaman, R., et al.Terconazole - a new broad-spectrum antifungalChemotherapy29(5)322-331(1983) 2.Vanden Bossche, H., and Marichal, P.Mode of action of anti-Candida drugs: Focus on terconazole and other ergosterol biosynthesis inhibitorsAm. J. Obstet. Gynecol.165(4 Pt 2)1193-1199(1991) 3.Isaacson, D.M., Tolman, E.L., Tobia, A.J., et al.Selective inhibition of 14α-desmethyl sterol synthesis in Candida albicans by terconazole, a new triazole antimycoticJ. Antimicrob. Chemother.21(3)333-343(1988)
| Cas No. | 67915-31-5 | SDF | |
| 别名 | 特康唑; R42470 | ||
| Canonical SMILES | CC(N1CCN(C2=CC=C(OC[C@@H]3O[C@@](CN4N=CN=C4)(C5=CC=C(Cl)C=C5Cl)OC3)C=C2)CC1)C | ||
| 分子式 | C26H31Cl2N5O3 | 分子量 | 532.46 |
| 溶解度 | DMSO : ≥ 30 mg/mL (56.34 mM) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8781 mL | 9.3904 mL | 18.7808 mL |
| 5 mM | 0.3756 mL | 1.8781 mL | 3.7562 mL |
| 10 mM | 0.1878 mL | 0.939 mL | 1.8781 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。
Double-blind investigation of R-42470 (Terconazole cream 0.4%) and clotrimazole (cream 1%) for the topical treatment of mycotic vaginitis
Chemioterapia 1984 Jun;3(3):192-5.PMID:6529776doi
A total of 78 patients took part in a double-blind randomized comparison of the efficacy, acceptability and tolerance of a new antifungal Terconazole (R-42470) (cream 0.4%) with the well established and clinically effective clotrimazole (cream 1%) for the topical treatment of mycotic vaginitis. Five grams of cream were applied to the vagina for 7 consecutive days. Twenty non-pregnant and 19 pregnant patients were included in each group. Clinical and mycological controls were carried out one week and one month after completion of therapy and 89.7% of the patients treated with Terconazole responded to therapy and 82.1% patients treated with clotrimazole were cured. Statistical analysis showed no significant difference when the results of the Terconazole treated patients and the clotrimazole group were compared.