Pivmecillinam hydrochloride (FL-1039 hydrochloride)
(Synonyms: 匹美西林盐酸盐; FL-1039 hydrochloride) 目录号 : GC32175
Pivmecillinam is a β-lactam antibiotic and a prodrug of mecillinam. It has selective activity against Gram-negative bacteria and is used primarily in the treatment of lower urinary tract infections.
Cas No.:32887-03-9
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
Pivmecillinam is a β-lactam antibiotic and a prodrug of mecillinam. It has selective activity against Gram-negative bacteria and is used primarily in the treatment of lower urinary tract infections.
| Cas No. | 32887-03-9 | SDF | |
| 别名 | 匹美西林盐酸盐; FL-1039 hydrochloride | ||
| Canonical SMILES | O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2/N=C/N3CCCCCC3)N1C2=O)OCOC(C(C)(C)C)=O.[H]Cl | ||
| 分子式 | C21H34ClN3O5S | 分子量 | 476.03 |
| 溶解度 | DMSO : ≥ 34 mg/mL (71.42 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。 |
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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 | 2.1007 mL | 10.5035 mL | 21.0071 mL |
| 5 mM | 0.4201 mL | 2.1007 mL | 4.2014 mL |
| 10 mM | 0.2101 mL | 1.0504 mL | 2.1007 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。
Stability-indicating assay for Pivmecillinam hydrochloride and Pivmecillinam hydrochloride capsules
J Chromatogr 1979 Oct 19;178(1):97-14.PMID:231046DOI:10.1016/s0021-9673(00)89700-9.
A high-pressure liquid chromatographic assay has been developed for Pivmecillinam hydrochloride and Pivmecillinam hydrochloride capsules. The method separates five reported degradation products and a number of esterified, related compounds. The accuracy of this method is comparable to the published ultraviolet assay and the relative standard deviation of a series of six replicate assays was better than +/- 0.7%.
LC-MS/MS methods for determination of unstable pivmecillinam and mecillinam in acidified human plasma: Application to a pharmacokinetic study
J Sep Sci 2022 Jul;45(14):2543-2554.PMID:35593582DOI:10.1002/jssc.202200070.
Pivmecillinam, the ester of biologically active antibiotic mecillinam, is an effective oral preparation to treat urinary tract infections. To study pharmacokinetics in humans, LC-MS/MS methods were developed to quantify pivmecillinam and mecillinam in human plasma, respectively. Considering cephalexin as internal standard, analytes were separated on UltimateXB-C18 columns after protein precipitation by acetonitrile. The mobile phase was composed of water containing 0.1% formic acid and methanol. The multiple reactions monitoring transitions of m/z 440.2→167.1, 326.1→167.1, and 348.1→158.1 were selected to inspect pivmecillinam, mecillinam, and the internal standard in positive ion mode. No apparent matrix effect was perceived. Linearities were obtained over calibration ranges of 0.0500-12.0 and 10.0-15,000 ng/mL, respectively. The intraday precisions were below 5.5%, the interday precisions were below 6.1%, and accuracies were within -8.1 to 13.0%. Stability tests were conducted and an acidification step was explored to enhance the stability of pivmecillinam and mecillinam. Further stability was validated under various storage and processing conditions. Both methods were applied to a pharmacokinetic study of pivmecillinam and mecillinam after oral administration of 400 mg Pivmecillinam hydrochloride tablets in healthy Chinese subjects.
Urinary excretion of mecillinam by volunteers receiving film-coated tablets of Pivmecillinam hydrochloride
Chemotherapy 1979;25(1):1-4.PMID:217572DOI:10.1159/000237814.
Mecillinam is a new amidinopenicillin which is taken orally as its ester pivmecillinam. 10 healthy volunteers were each given 200 mg of Pivmecillinam hydrochloride four times daily and all urine was collected and cooled to -20 degrees C to minimize antibiotic degradation. 43% of the ingested antibiotic was recovered from the urine in its microbiologically active form, during the first 12 h and 34% during the subsequent 24 h. The corresponding figures for 10 volunteers receiving double this dose of antibiotic was 30 and 34%. The mean half life of mecillinam in urine due to spontaneous breakdown at 37 degrees C was 17 h. There was evidence that stearate-film-coated Pivmecillinam hydrochloride tablets may be less likely to cause dyspepsia than gelatine capsules.