Rifampicin-d3
(Synonyms: 利福平 d3) 目录号 : GC48048
An internal standard for the quantification of rifampicin
Cas No.:1262052-36-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rifampicin-d3 is intended for use as an internal standard for the quantification of rifampicin by GC- or LC-MS. Rifampicin is a rifamycin antibiotic and inhibitor of bacterial RNA polymerase (IC50 = 0.01 μg/ml for the E. coli enzyme).1 It inhibits the growth of M. tuberculosis H37Rv in mouse peritoneal macrophages (MIC = 0.8 μg/ml) as well as clinical isolates of various species of Staphylococcus, Streptococcus, Haemophilus, and Neisseria (MICs = 0.009-1.4 μg/ml).2,3 Rifampicin increases survival in a mouse model of tuberculosis infection.3 It is also an agonist of the human pregnane X receptor (PXR; EC50 = ~2 μM).4 Formulations containing rifampicin have been used in the treatment of tuberculosis and meningococcal carriers.
1.Wehrli, W.Rifampin: Mechanisms of action and resistanceRev.Infect.Dis.5(3)S407-S411(1983) 2.Jhamb, S.S., Goyal, A., and Singh, P.P.Determination of the activity of standard anti-tuberculosis drugs against intramacrophage Mycobacterium tuberculosis, in vitro: MGIT 960 as a viable alternative for BACTEC 460Braz. J. Infect. Dis.18(3)336-340(2014) 3.Arioli, V., Berti, M., Carniti, G., et al.Antibacterial activity of DL 473, a new semisynthetic rifamycin derivativeJ. Antibiot. (Tokyo)34(8)1026-1032(1981) 4.Gill, S.K., Xu, H., Kirchhoff, P.D., et al.Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerasesJournal of Medicinal Chemistry55(8)3814-3826(2012)
| Cas No. | 1262052-36-7 | SDF | |
| 别名 | 利福平 d3 | ||
| Canonical SMILES | OC1=C2C(C(O)=C(C)C(O[C@]3(C)O/C=C/[C@H](OC)[C@H](C)[C@]([C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)/C=C/C=C(C)/C(N4)=O)(OC(C)=O)[H])=C2C3=O)=C(O)C4=C1/C=N/N5CCN(C([2H])([2H])[2H])CC5 | ||
| 分子式 | C43H55D3N4O12 | 分子量 | 826 |
| 溶解度 | Chloroform: slightly soluble,Methanol: slightly soluble | 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 | 1.2107 mL | 6.0533 mL | 12.1065 mL |
| 5 mM | 0.2421 mL | 1.2107 mL | 2.4213 mL |
| 10 mM | 0.1211 mL | 0.6053 mL | 1.2107 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。
Validation and application of a quantitative liquid chromatography tandem mass spectrometry assay for the analysis of rifapentine and 25-O-desacetyl rifapentine in human milk
J Pharm Biomed Anal 2022 Jun 5;215:114774.PMID:35462285DOI:PMC9871952
A robust analytical method based on liquid chromatography coupled to tandem mass spectrometry was developed and validated to quantify rifapentine and 25-O-desacetyl rifapentine in human breast milk to aid in determining the breastfed infant risk to the excreted drug in human milk. Samples were extracted by a combination of protein precipitation and solid phase extraction using Rifampicin-d3 as an internal standard. An Agilent® Poroshell 120 EC-C18 (4.6 mm × 50 mm, 2.7 µm) column was used for chromatographic separation employing an isocratic mobile phase consisting of acetonitrile: methanol: 0.1% formic acid (55/5/40, v/v/v) at a flow rate of 450 µL/min, and with a total run time of four minutes. Mass detection was on an AB Sciex API 4000 mass spectrometer using electrospray ionization in the positive mode and based on multiple reaction monitoring data acquisition. Rifapentine was accurately quantified across a concentration range of 2.00-2000 ng/mL and 25-O-desacetyl rifapentine from 4.00 to 2000 ng/mL. During validation, the inter- and intra-day accuracy and precision at the tested QC concentrations (N = 18) for rifapentine were between 97.4% and 100.6%, and 3.1% and 8.3%, respectively. The inter- and intra-day accuracy and precision for 25-O-desacetyl rifapentine were between 96.4% and 106.3%, and 6.7% and 11.8%, respectively. No significant matrix effects were observed, and the method was shown to be specific for rifapentine and 25-O-desacetyl rifapentine. Human milk samples (N = 22) generated during a phase I/II clinical trial were successfully analysed for rifapentine and 25-O-desacetyl rifapentine using this validated method. Concentrations for rifapentine and 25-O-desacetyl rifapentine in human milk samples (N = 22) ranged from 11.2-1180 ng/mL and 7.11-573 ng/mL, respectively.