Cefpirome sulfate (HR-810 sulfate)
(Synonyms: 硫酸头孢匹罗; HR-810 sulfate) 目录号 : GC32154
Cefpirome(HR-810 sulfate) is a fourth-generation cephalosporin and is considered highly active against Gram-negative bacteria.
Cas No.:98753-19-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefpirome(HR-810 sulfate) is a fourth-generation cephalosporin and is considered highly active against Gram-negative bacteria.
| Cas No. | 98753-19-6 | SDF | |
| 别名 | 硫酸头孢匹罗; HR-810 sulfate | ||
| Canonical SMILES | O=C1[C@@H](NC(/C(C2=CSC(N)=N2)=N\OC)=O)[C@@]3([H])SCC(C[N+]4=CC=CC5=C4CCC5)=C(C(O)=O)N13.O=S(O)([O-])=O | ||
| 分子式 | C22H24N6O9S3 | 分子量 | 612.66 |
| 溶解度 | Water : 5 mg/mL (8.16 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| 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。 |
||
| 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 | 1.6322 mL | 8.1611 mL | 16.3223 mL |
| 5 mM | 0.3264 mL | 1.6322 mL | 3.2645 mL |
| 10 mM | 0.1632 mL | 0.8161 mL | 1.6322 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 and degradation pattern of cefpirome (HR 810) in aqueous solution
Chem Pharm Bull (Tokyo) 1990 Jul;38(7):1998-2002.PMID:2268903DOI:10.1248/cpb.38.1998.
The stability and degradation pathways of a new semi-synthetic cephalosporin, 1-[[(6R,7R)-7-[2-(2-amino-4-thiazolyl)glyoxylamido]-2-carboxy-8-ox o-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-6,7-dihydro-5H-1- pyridinium hydroxide, inner salt, 7(2)-(Z)-(O-methyloxime) sulfate (Cefpirome sulfate, HR 810), were studied. Cefpirome in various buffer solutions was allowed to stand at 40 degrees C and its degradation patterns were investigated by high performance liquid chromatography. Cefpirome was stable in the region of pH 4-7 and slightly unstable beyond this range. In aqueous solution from the neutral to alkaline regions, the produced degradation products were: 1- [[(6R,7S)-7-[2-(2-amino-4-thiazolyl)glyoxylamido]-2-carboxy-8-oxo -5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-6,7-dihydro-5 H-1- pyridinium hydroxide, inner salt, 7(2)-(Z)-(O-methyloxime) (epi-cefpirome); 1-[[(6R,7R)-7-[2-(2-amino-4-thiazolyl)glyoxylamido]-2-carboxy-8-ox o-5-thia-1-azabicyclo[4.2.0]oct-3-en-3-yl]methyl]-6,7-dihydro-5H-1- pyridinum hydroxide, inner salt, 7(2)-(Z)-(O-methyloxime) (delta 2-cefpirome); 2-[[(2-amino-4-thiazolyl)((Z)-methoxy-imino)acetyl]amino]acetaldehyde; and 6,7-dihydro-5H-1-pyrindine. On the other hand, 1-[[(6R,7R)-7-[2-(2- amino-4-thiazolyl)glyoxylamido]-2-carboxy-8-oxo-5-thia-1- azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-6,7-dihydro-5H-1-pyridinium++ + hydroxide, inner salt, 7(2)-(E)-(O-methyloxime) (anti-cefpirome), 2-[[(2- amino-4-thiazolyl)-((Z)-methoxyimino)-acetyl]aminomethyl]-1,2,5,7- tetrahydro-7-oxo-4H-furo[3,4-D]-[1,3]thiazine, and 6,7-dihydro-5H-1- pyrindine were produced in strongly acidic solution or under irradiation by artificial sunlight.
The radiolytic studies of Cefpirome sulfate in the solid state
J Pharm Biomed Anal 2016 Jan 25;118:410-416.PMID:26597316DOI:10.1016/j.jpba.2015.11.008.
The possibility of applying radiation sterilization to Cefpirome sulfate was investigated. The lack of changes in the chemical structure of Cefpirome sulfate irradiated with a dose of 25 kGy, required to attain sterility, was confirmed by UV, FT-IR, Raman, DSC and chromatographic methods. Some radical defects with concentration no more than over a several dozen ppm were created by radiation. The antibacterial activity of Cefpirome sulfate for two Gram-positive and three Gram-negative strains was changed. The radiation sterilised Cefpirome sulfate was not in vitro cytotoxic against fibroblast cells.
STABILITY OF Cefpirome sulfate IN AQUEOUS SOLUTIONS
Acta Pol Pharm 2016 Jan-Feb;73(1):23-7.PMID:27008797doi
The influence of pH on the stability of Cefpirome sulfate was investigated in the pH range of 0.44 - 13.00. The degradation of Cefpirome sulfate as a result of hydrolysis was a pseudo-first-order reaction. General acid-base hydrolysis of Cefpirome sulfate was not observed. In the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffer, k(obs) = k(pH) because specific acid-base catalysis was observed. Specific acid-base catalysis of Cefpirome sulfate consisted of the following reactions: hydrolysis of Cefpirome sulfate catalyzed by hydrogen ions (kH+), hydrolysis of dications (k₁H₂O) monocations (k₿H₂O), zwitter ions (k₃H₂O) and monoanions (k₿H₂O) of Cefpirome sulfate under the influence of water. The total rate of the reaction was equal to the sum of partial reactions k(pH) = kH+ x aH+ + kH₂O x f₿+ k₂H₂O x f₿+ k₃H₂O x f₿+ k₿H₂O x f₿ Based on the dependence k(pH) = f(pH) it was found that Cefpirome sulfate was the most stable in aqueous solutions in the pH range of 4-6.
Separation and characterization of impurities and isomers in Cefpirome sulfate by liquid chromatography/tandem mass spectrometry and a summary of the fragmentation pathways of oxime-type cephalosporins
Rapid Commun Mass Spectrom 2021 Feb 28;35(4):e9004.PMID:33188542DOI:10.1002/rcm.9004.
Rationale: Although the identification of degradation products of Cefpirome sulfate has been reported, there has been no report concerning the impurities in bulk samples of this compound. To meet the requirements of the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use, the structures of impurities whose content are over 0.1% need to be confirmed. Thus, characterization of the impurities in Cefpirome sulfate bulk samples is critical for controlling the production of this drug. Methods: The structures of Cefpirome sulfate impurities were investigated using two-dimensional liquid chromatography (LC) coupled to electrospray ionization tandem mass spectrometry. In the first LC dimension, a Kromasil 100-5C18 column (4.6 mm × 250 mm, 5 μm) was used, and the mobile phases were 0.03 M ammonium dihydrogen phosphate solution and acetonitrile. In the second dimension, the column was a Shimadzu Shim-pack GISS C18 column (50 mm × 2.1 mm, 1.9 μm), and the mobile phases were 10 mM ammonium formate solution and methanol. An ion trap time-of-flight mass spectrometer operated in both positive and negative ion mode was employed in this study. Results: Nine impurities and isomers in Cefpirome sulfate, eight of which were previously unknown, were separated and characterized. Structures were proposed for the eight unknown compounds based on the MSn fragmentation data. The degradation behavior of Cefpirome sulfate was also studied. Conclusions: Based on the characterization of impurities and isomers, this study could be used to improve the quality control of the Cefpirome sulfate drug recommended in pharmacopoeias. The degradation behavior of Cefpirome sulfate provides a basis for the selection of storage conditions.
Investigation on the interaction of Cefpirome sulfate with lysozyme by fluorescence quenching spectroscopy and synchronous fluorescence spectroscopy
Luminescence 2016 Mar;31(2):580-586.PMID:26304690DOI:10.1002/bio.2998.
The reaction mechanism of Cefpirome sulfate with lysozyme at different temperatures (298, 310 and 318 K) was investigated using fluorescence quenching and synchronous fluorescence spectroscopy under simulated physiological conditions. The results clearly demonstrated that Cefpirome sulfate caused strong quenching of the fluorescence of lysozyme by a static quenching mechanism. The binding constants obtained using the above methods were of the same order of magnitude and very similar. Static electric forces played a key role in the interaction between Cefpirome sulfate and lysozyme, and the number of binding sites in the interaction was close to 1. The values of Hill's coefficients were > 1, indicating that drugs or proteins showed a very weakly positive cooperativity in the system. In addition, the conclusions obtained from the two methods using the same equation were consistent. The results indicated that synchronous fluorescence spectrometry could be used to study the binding mechanism between drug and protein, and was a useful supplement to the fluorescence quenching method. In addition, the effect of Cefpirome sulfate on the secondary structure of lysozyme was analyzed using circular dichroism spectroscopy.