Dalbavancin hydrochloride
(Synonyms: 盐酸达巴万星; MDL-63397 hydrochloride; BI-397 hydrochloride) 目录号 : GC60739A semisynthetic glycopeptide antibiotic
Cas No.:2227366-51-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dalbavancin is a semisynthetic glycopeptide antibiotic.1 It inhibits the growth of Gram-positive bacteria in vitro, including S. pneumoniae, S. pyogenes, vancomycin-sensitive Enterococcus species, and various methicillin-resistant staphylococci (MIC50s = 0.03, ≤0.002, 0.13, and 0.03-0.13 mg/L, respectively). Dalbavancin increases survival in mouse models of infection with S. aureus and S. pneumoniae (ED50s = 0.08 and 0.56 mg/kg, respectively). This product is a mixture of five closely related components, dalbavancin A0, A1, B0, B1, and B2, with dalbavancin B0 being the major component (≥75%). Formulations containing dalbavancin have been used in the treatment of bacterial skin infections caused by Gram-positive bacteria.
1.Candiani, G., Abbondi, M., Borgonovi, M., et al.In-vitro and in-vivo antibacterial activity of BI 397, a new semi-synthetic glycopeptide antibioticJ. Antimicrob. Chemother.44(2)179-192(1999)
Cas No. | 2227366-51-8 | SDF | |
别名 | 盐酸达巴万星; MDL-63397 hydrochloride; BI-397 hydrochloride | ||
Canonical SMILES | O[C@@H]([C@@H](O)[C@@H]1O)[C@H](O[C@@H]1CO)OC2=C(C3=CC([C@@](C4=O)([H])NC([C@@](NC([C@](NC([C@@](NC5=O)([H])C6)=O)([H])C(C=C7OC(C=C8[C@H]5NC)=C(C=C8)O)=C(C(O)=C7)Cl)=O)([H])C9=CC%10=C(O[C@H](O[C@H](C(O)=O)[C@@H](O)[C@@H]%11O)[C@@H]%11NC(CCCCCCCCC(C)C)=O)C(OC%12=CC=C6C=C%12)=C9)=O)=CC=C3O)C([C@@](NC([C@](N4)([H])[C@@H](C%13=CC=C(O%10)C(Cl)=C%13)O)=O)([H])C(NCCCN(C)C)=O)=CC(O)=C2.[H]Cl | ||
分子式 | C88H101Cl3N10O28 | 分子量 | 1853.15 |
溶解度 | Water: 50 mg/mL (26.98 mM); DMSO: ≥ 24 mg/mL (12.95 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.5396 mL | 2.6981 mL | 5.3962 mL |
5 mM | 0.1079 mL | 0.5396 mL | 1.0792 mL |
10 mM | 0.054 mL | 0.2698 mL | 0.5396 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。
A Systematic Degradation Kinetics Study of Dalbavancin hydrochloride Injection Solutions
J Pharm Sci 2023 Feb 12;S0022-3549(23)00057-6.PMID:36780988DOI:10.1016/j.xphs.2023.02.006.
The degradation kinetics of the glycopeptide antibiotic dalbavancin in solution are systematically evaluated over the pH range 1-12 at 70°C. The decomposition rate of dalbavancin was measured as a function of pH, buffer composition, temperature, ionic strength, and drug concentration. A pH-rate profile was constructed using pseudo first-order kinetics at 70°C after correcting for buffer effects; the observed pH-rate profile could be fitted with standard pseudo first order rate laws. The degradation reactions of dalbavancin were found to be strongly dependent on pH and were catalyzed by protons or hydroxyl groups at extreme pH values. Dalbavancin shows maximum stability in the pH region 4-5. Based on the Arrhenius equation, dalbavancin solution at pH 4.5 is predicted to have a maximum stability of thirteen years under refrigerated conditions, eight months at room temperature and one month at 40°C. Mannosyl Aglycone (MAG), the major thermal and acid degradation product, and DB-R6, an additional acid degradation product, were formed in dalbavancin solutions at 70°C due to hydrolytic cleavage at the anomeric carbons of the sugars. Through deamination and hydrolytic cleavage of dalbavancin, a small amount of DB-Iso-DP2 (RRT-1.22) degradation product was also formed under thermal stress at 70°C. A greater amount of the base degradation product DB-R2 forms under basic conditions at 70°C due to epimerization of the alpha carbon of phenylglycine residue 3.
Simultaneous Quantification and Pharmacokinetic Study of Five Homologs of Dalbavancin in Rat Plasma Using UHPLC-MS/MS
Molecules 2020 Sep 8;25(18):4100.PMID:32911715DOI:10.3390/molecules25184100.
Dalbavancin is a novel semisynthetic glycopeptide antibiotic that comprises multiple homologs and isomers of similar polarities. However, pharmacokinetic studies have only analyzed the primary components of dalbavancin, namely B0 and B1. In this study, an ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed to simultaneously determinate and investigate the five homologous components of dalbavancin, namely, A0, A1, B0, B1, and B2, in rat plasma. In this method, methanol was used to precipitate plasma, and a triple-bonded alkyl chromatographic column was used for molecule separation, using 0.1% formic acid-acetonitrile as the mobile phase for gradient elution. Targeted homologs were analyzed by a triple quadrupole mass spectrometer using positive electrospray ionization in multiple reaction monitoring mode. The linearity range was 50-2500 ng/mL with a high correlation coefficient (r2 > 0.998). This method was successfully applied in the pharmacokinetic analysis of Dalbavancin hydrochloride to investigate dalbavancin components in rats.