Posaconazole-D4
(Synonyms: 泊沙康唑-D5,SCH 56592-d4) 目录号 : GC61204
Posaconazole-D4是Posaconazole的氘化标记形式。Posaconazole是一种广谱的，二代三唑类物质，具有抗真菌作用。
Cas No.:1133712-26-1
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
Posaconazole-D4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
[1]. Herbrecht R, et al. Management of systemic fungal infections: alternatives to itraconazole. J Antimicrob Chemother. 2005 Sep;56 Suppl 1:i39-i48.
| Cas No. | 1133712-26-1 | SDF | |
| 别名 | 泊沙康唑-D5,SCH 56592-d4 | ||
| Canonical SMILES | FC1=CC=C([C@@]2(CN3C=NC=N3)C[C@H](COC4=CC=C(N5CCN(C6=C([2H])C([2H])=C(N7C=NN([C@@H](CC)[C@H](C)O)C7=O)C([2H])=C6[2H])CC5)C=C4)CO2)C(F)=C1 | ||
| 分子式 | C37H38D4F2N8O4 | 分子量 | 704.8 |
| 溶解度 | DMSO : 18.75 mg/mL (26.60 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4188 mL | 7.0942 mL | 14.1884 mL |
| 5 mM | 0.2838 mL | 1.4188 mL | 2.8377 mL |
| 10 mM | 0.1419 mL | 0.7094 mL | 1.4188 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。
Liquid chromatography-mass spectrometry method for the quantification of posaconazole in human plasma: application to pharmacokinetics following single-dose administration in the fasted state and with a high-fat meal
Pharmazie 2013 Mar;68(3):173-7.PMID:23556334doi
A liquid chromatography/tandem mass spectrometry (LC-MS/MS) method was developed to determine concentrations of posaconazole in human plasma precipitated by acetonitrile including internal standard. Rapid chromatographic separation was achieved in the mobile phase composition of acetonitrile, water and formic acid (v/v/v, 55:45:0.1) with a flow rate of 0.25 ml/min. Posaconazole-D4 was used as internal standard. Detection was undertaken with cation electrospray tandem mass spectrometry on a Sciex/API3000. The method was accurate, specific and sensitive for the analysis of posaconazole in human plasma in the concentration range of 2-1000 ng/ml. The inter- and intra-batch accuracy was within +/- 10% and the lower limit of quantification was 2 ng/ml. The method facilitated a clinical pharmacokinetic study after oral administration of a single-dose of posaconazole suspension in the fasted state and with a high-fat meal in a two-period crossover design. Cmax (maximum concentration) and AUC (area under serum drug concentration) were significantly increased, and Tmax (time to maximum plasma concentration) was delayed under fed condition, which suggested that simultaneous administration of posaconazole with food may help to achieve higher plasma concentrations and result in better antifungal efficacy.