Saperconazole (R66905)
(Synonyms: 沙康唑; R66905) 目录号 : GC32374
Saperconazole (R66905) (R66905) 是一种广谱抗真菌三唑类，对曲霉具有有效的活性，MIC90 为 0.19 mg/L。
Cas No.:110588-57-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | A total of 279 Aspergillus isolates are tested in vitro; 221 of these are A. fumigatus. The inoculum consists of a standardized 4 mm2 culture block containing hyphae and spores for tubes with 5 mL of medium supplemented with drug solution or with solvent[2]. |
Animal experiment: | Male immunocompetent (normal) or immunocompromised pigs weighing 500 g (±50 g) are infected intravenously (i.v.) with 25,000 CFU of A.fumigatus B19119 per g of body weight. The animals are treated orally with Saperconazole, ketoconazole, or fluconazole dissolved in polyethylene glycol 200 (PEG 200). The treatment is given once daily for 14 consecutive days, starting on the day of infection or on day 1, 2, 3, or 4 after infection. Saperconazole, dissolved in dimethyl-β-cyclodextrin and in hydroxypropyl-β-cyclodextrin is also administered i.p. and i.v. Pigeons with a mean weight of 400 g (±30 g) are infected i.v. in a wing vein with 7,800 CFU of A.fumigatus B19119 per g of body weight. Saperconazole dissolved in PEG 200 is administered by gavage at 0, 2.5, 5, or 10 mg/kg starting on the day of infection and continued once daily for 14 consecutive days[2]. |
References: [1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. | |
Saperconazole (R66905) is a broad-spectrum antifungal triazole and has potent activity against Aspergillus with an MIC90 of 0.19 mg/L.
The antifungal activity of Saperconazole is complete at 1 μg/mL for all but one strain of A. niger. Eighty percent of all strains show complete absence of growth at 0.1 μg/mL (85% for A. fumigatus), and this result persists during 14 days of the test[2].
All control pigeons infect with A. fumigatus die within 2 to 5 days. They have necrotic foci in the lungs, air sacs, liver, spleen, and kidneys. These organs are highly positive by histology and oncultures. Saperconazole administered at 2.5 mg/kg is not active, but when it is given at 5 or 10 mg/kg, 92 or 100%, respectively, survive and organ cultures are negative. No drug-related side effects are observed in the pigeons[2].
[1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. [2]. VVan Cutsem J, et al. Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals. Antimicrob Agents Chemother. 1989 Dec;33(12):2063-8.
| Cas No. | 110588-57-3 | SDF | |
| 别名 | 沙康唑; R66905 | ||
| Canonical SMILES | O=C1N(C(C)CC)N=CN1C2=CC=C(N3CCN(C4=CC=C(OCC5OC(CN6N=CN=C6)(C7=CC=C(F)C=C7F)OC5)C=C4)CC3)C=C2 | ||
| 分子式 | C35H38F2N8O4 | 分子量 | 672.72 |
| 溶解度 | DMSO : 25 mg/mL (37.16 mM; ultrasonic and warming and heat to 60°C) | 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 | 1.4865 mL | 7.4325 mL | 14.865 mL |
| 5 mM | 0.2973 mL | 1.4865 mL | 2.973 mL |
| 10 mM | 0.1487 mL | 0.7433 mL | 1.4865 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。
Saperconazole in the treatment of systemic and subcutaneous mycoses
Int J Dermatol 1992 Oct;31(10):725-9.PMID:1399205DOI:10.1111/j.1365-4362.1992.tb01384.x
In a 2-year period, 30 patients with culture-proven mycoses (chromoblastomycosis, sporotrichosis, and paracoccidioidomycosis) were treated with the new orally administered triazole, Saperconazole (SPZ) (R66905). The daily dose varied from 100 to 200 mg. All patients responded to treatment; the mean time required to heal the lesions and convert the cultures to negative was 3.5 months for sporotrichosis, 4.6 for paracoccidioidomycosis, and 9.0 for chromoblastomycosis. Evaluation by a scoring system indicated that 36.6% of the patients achieved complete resolution of the pretherapy abnormalities, while the remaining (63.3%) experienced major improvement. No collateral effects were reported; there were no bone-marrow or liver toxicities. SPZ is an effective drug for the treatment of the above-mentioned mycoses and appears to be suitable for the control of chromoblastomycosis.