| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| 体外研究 (In Vitro) |
达克宁是一种外用咪唑抗真菌药物,由杨森制药公司生产,用于治疗皮肤或粘膜的真菌感染。麦角甾醇是真菌细胞膜的重要组成部分,其通过阻止其形成而发挥作用。此外,它还用于对抗某些利什曼原虫,这是一种单细胞寄生虫,其细胞膜也含有麦角甾醇。除了抗真菌和抗寄生虫作用外,它还具有一定的抗菌特性。在柯达 E-6 工艺的最终处理过程以及类似的富士 CR-56 工艺中,咪康唑还被用作 Ektachrome 胶片开发过程中的甲醛替代品。在其 C-41RA Quick Access 彩色负片显影过程的成分中,Fuji Hunt 还加入了达克康唑作为最终冲洗成分。
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|---|---|
| 药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Following a single oral dose of 50 mg miconazole tablets in healthy volunteers, the mean Cmax was 15.1 ± 16.2 mcg/mL, the mean AUC0-24 was 55.2 ± 35.1 mcgh/mL, and the median Tmax was 7 hours (range 2.0–24.1 hours). Measurable plasma concentrations in these patients ranged from 0.5 to 0.83 mcg/mL. Topically applied miconazole showed poor absorption into the systemic circulation. In pediatric patients aged 1–21 months, after multiple topical applications of miconazole ointment over 7 consecutive days, 88% of patients had plasma miconazole concentrations below 0.5 ng/mL, while the remaining patients had concentrations of 0.57 ng/mL and 0.58 ng/mL, respectively. Similarly, [the text abruptly ends here, likely due to an incomplete sentence or missing information]. Following administration of a 1200 mg vaginal suppository, the mean Cmax was 10.71 ng/mL, the mean Tmax was 18.4 hours, and the mean AUC0-96 was 477.3 ngh/mL. Miconazole is primarily excreted via urine and feces; less than 1% of unmetabolized miconazole is recovered in urine. The calculated apparent volume of distribution (VOD) of the 1200 mg miconazole vaginal suppository is 95,546 L, while that of the 100 mg vaginal cream is 10,911 L. Metabolites/Metabolites: Miconazole is metabolized in the liver without producing any active metabolites. Biological Half-Life: The terminal half-life of miconazole is 24 hours. |
| 毒性/毒理 (Toxicokinetics/TK) |
Toxicity Summary
Miconazole interacts with 14α-demethylase, a cytochrome P-450 enzyme essential for the conversion of lanosterol to ergosterol. Since ergosterol is a crucial component of the fungal cell membrane, inhibition of its synthesis leads to increased cell permeability, resulting in leakage of cell contents. Miconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit yeast conversion to mycelium, inhibit purine uptake, and impair the biosynthesis of triglycerides and/or phospholipids. Toxicity Data LD50: 3800 mg/kg (oral, mouse) (A308) LD50: 3 g/kg (oral, rat) (A308) |
| 参考文献 | |
| 其他信息 |
Pharmacodynamics
Miconazole is an azole antifungal drug whose main mechanism of action is by inhibiting specific demethylases in the CYP450 complex. Because miconazole is usually applied topically and is minimally absorbed into the systemic circulation after administration, most adverse reactions in patients are limited to hypersensitivity reactions and anaphylactic shock. Patients using vaginal miconazole preparations are advised not to rely on contraception to prevent pregnancy and sexually transmitted infections, and should not use tampons concurrently. |
| 分子式 |
C18H14CL4N2O
|
|---|---|
| 分子量 |
416.13
|
| 精确质量 |
413.986
|
| CAS号 |
22916-47-8
|
| 相关CAS号 |
Miconazole nitrate;22832-87-7;Miconazole-d5;1216653-50-7;Miconazole-d5 nitrate;1216653-51-8;Miconazole-d2;2140316-33-0
|
| PubChem CID |
4189
|
| 外观&性状 |
White to off-white solid powder
|
| 密度 |
1.4±0.1 g/cm3
|
| 沸点 |
555.1±50.0 °C at 760 mmHg
|
| 熔点 |
159-163ºC
|
| 闪点 |
289.5±30.1 °C
|
| 蒸汽压 |
0.0±1.4 mmHg at 25°C
|
| 折射率 |
1.625
|
| LogP |
5.93
|
| tPSA |
27.05
|
| 氢键供体(HBD)数目 |
0
|
| 氢键受体(HBA)数目 |
2
|
| 可旋转键数目(RBC) |
6
|
| 重原子数目 |
25
|
| 分子复杂度/Complexity |
417
|
| 定义原子立体中心数目 |
0
|
| InChi Key |
BYBLEWFAAKGYCD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H14Cl4N2O/c19-13-2-1-12(16(21)7-13)10-25-18(9-24-6-5-23-11-24)15-4-3-14(20)8-17(15)22/h1-8,11,18H,9-10H2
|
| 化学名 |
1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole
|
| HS Tariff Code |
2934.99.9001
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外实验) |
DMSO : 100 mg/mL (240.31 mM)
|
|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (6.01 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: 2.08 mg/mL (5.00 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 悬浊液; 超声助溶。 例如,若需制备1 mL的工作液,可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.08 mg/mL (5.00 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4031 mL | 12.0155 mL | 24.0310 mL | |
| 5 mM | 0.4806 mL | 2.4031 mL | 4.8062 mL | |
| 10 mM | 0.2403 mL | 1.2015 mL | 2.4031 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。