Diniconazole (Rac-diniconazole)
(Synonyms: 烯唑醇; Rac-diniconazole) 目录号 : GC32151A triazole fungicide
Cas No.:83657-24-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Diniconazole is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death.1 It is fungicidal against B. cinerea, S. fimicola, F. graminearum, S. cepivorum, and B. sorokiniana (EC50s = 0.012, <0.001, 0.008, 0.02, and 0.06 mg/l, respectively).2 Diniconazole acts as a plant growth regulator, decreasing height and leaf area in bean plants when applied to roots at a concentration of 5 mg/l. It exhibits dose-dependent toxicity in zebrafish.3
1.Yoshida, Y., Aoyama, Y., Takano, H., et al.Stereo-selective interaction of enantiomers of diniconazole, a fungicide, with purified P-450/14DM from yeastBiochem. Biophys. Res. Commun.137(1)513-519(1986) 2.Fletcher, R.A., Hofstra, G., and Gao, J.Comparative fungitoxic and plant growth regulating properties of triazole derivativesPlant Cell Physiol.27(2)367–371(1986) 3.Jing, G., Wen-hua, S., Feng, D., et al.Acute toxicity study on zebrafish (Danio rerio) exposure to triazole fungicidesJ. SE Univ. (Med. Sci. Ed.)29(4)402-406(2010)
Cas No. | 83657-24-3 | SDF | |
别名 | 烯唑醇; Rac-diniconazole | ||
Canonical SMILES | OC(C(C)(C)C)/C(N1N=CN=C1)=C\C2=CC=C(Cl)C=C2Cl | ||
分子式 | C15H17Cl2N3O | 分子量 | 326.22 |
溶解度 | DMSO : ≥ 100 mg/mL (306.54 mM);Water : < 0.1 mg/mL (insoluble) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0654 mL | 15.3271 mL | 30.6542 mL |
5 mM | 0.6131 mL | 3.0654 mL | 6.1308 mL |
10 mM | 0.3065 mL | 1.5327 mL | 3.0654 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。
Stereoselective pharmacokinetics of diniconazole enantiomers in rabbits
Chirality 2009 Jul;21(7):699-703.PMID:18973222DOI:10.1002/chir.20667
Diniconazole [(E)-(RS)-1-(2,4,-dichlorophenyl)-4,4-dimethyl-2-(1H-1,2,4-triazole-1-yl)pent-1-en-3-ol)] is a potent triazole fungicide. The enantioselective pharmacokinetics of diniconazole enantiomers in rabbits was studied via intravenous (i.v.) injection. The pharmacokinetics and the enantiomer fraction (EF) were determined using normal high-performance liquid chromatography with diode array detection and a cellulose-tris-(3,5-dimethylphenylcarbamate)-based chiral stationary phase (CDMPC-CSP). The time-concentration curves in plasma were fitted by a two-compartment open mode. The results showed that the concentration of S-diniconazole in plasma decreased faster than that of R-diniconazole, and EFs increased with time after administration of racemic Diniconazole (Rac-diniconazole). The R-/S-enantiomer ratio of the area under the time-plasma concentration curve (AUC(0-infinity)) after administration was 1.52. The total plasma clearance value of S-enantiomer was 1.57-fold higher than that of the R-diniconazole. These results indicate substantial stereoselectivity in the kinetics of diniconazole enantiomers in rabbit.