Clindamycin Sulfoxide
(Synonyms: 克林霉素亚砜) 目录号 : GC43278
An active metabolite of clindamycin
Cas No.:22431-46-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Clindamycin sulfoxide is an active metabolite of the antibiotic clindamycin . It is formed via S-oxidation of clindamycin primarily by the cytochrome P450 (CYP) isoform CYP3A4. Clindamycin sulfoxide inhibits the growth of P. prevotti, B. fragilis, and C. sordelli in vitro with MIC values of 2, 2, and 1 mg/L, respectively.
| Cas No. | 22431-46-5 | SDF | |
| 别名 | 克林霉素亚砜 | ||
| Canonical SMILES | O=C(N[C@@]([C@H](C)Cl)([H])[C@@]1([H])O[C@@](S(C)=O)([H])[C@H](O)[C@@H](O)[C@H]1O)[C@H]2N(C)C[C@H](CCC)C2 | ||
| 分子式 | C18H33ClN2O6S | 分子量 | 441 |
| 溶解度 | Methanol: Slightly Soluble,Water: 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 | 2.2676 mL | 11.3379 mL | 22.6757 mL |
| 5 mM | 0.4535 mL | 2.2676 mL | 4.5351 mL |
| 10 mM | 0.2268 mL | 1.1338 mL | 2.2676 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。
Determination of clindamycin and its metabolite Clindamycin Sulfoxide in diverse sewage samples
Environ Sci Pollut Res Int 2014 Oct;21(20):11764-9.PMID:24310902DOI:10.1007/s11356-013-2333-2.
In a research project on risk management of harmful substances in water cycles, clindamycin and 12 further antibiotics were determined in different sewage samples. In contrast to other antibiotics, an increase of the clindamycin concentration in the final effluent in comparison to the influent of the sewage treatment plant (STP) was observed. A back transformation from the main metabolite Clindamycin Sulfoxide to clindamycin during the denitrification process has been discussed. Therefore, the concentration of this metabolite was measured additionally. Clindamycin Sulfoxide was stable in the STP and the assumption of back transformation of the metabolite to clindamycin was confuted. To explain the increasing clindamycin concentration in the STP, the ratio of Clindamycin Sulfoxide to clindamycin was observed. The ratio increased in dry spells with concentrated samples and with long dwell time in the sewer system. A short hydraulic retention in waste water system and diluted samples in periods of extreme rainfall lead to a lower ratio of Clindamycin Sulfoxide to clindamycin concentration. A plausible explanation of this behavior could be that clindamycin was adsorbed strongly to a component of the sewage during this long residence time and in the STP, clindamycin was released. In the common sample preparation in the lab, clindamycin was not released. Measurements of clindamycin and Clindamycin Sulfoxide in the influent and effluent of STP is advised for sewage monitoring.
Transformation products of clindamycin in moving bed biofilm reactor (MBBR)
Water Res 2017 Apr 15;113:139-148.PMID:28213335DOI:10.1016/j.watres.2017.01.058.
Clindamycin is widely prescribed for its ability to treat a number of common bacterial infections. Thus, clindamycin enters wastewater via human excretion or disposal of unused medication and widespread detection of pharmaceuticals in rivers proves the insufficiency of conventional wastewater treatment plants in removing clindamycin. Recently, it has been discovered that attached biofilm reactors, e.g., moving bed biofilm reactors (MBBRs) obtain a higher removal of pharmaceuticals than conventional sludge wastewater treatment plants. Therefore, this study investigated the capability of MBBRs applied in the effluent of conventional wastewater treatment plants to remove clindamycin. First, a batch experiment was executed with a high initial concentration of clindamycin to identify the transformation products. It was shown that clindamycin can be removed from wastewater by MBBR and the treatment process converts clindamycin into the, possibly persistent, products Clindamycin Sulfoxide and N-desmethyl clindamycin as well as 3 other mono-oxygenated products. Subsequently, the removal kinetics of clindamycin and the formation of the two identified products were investigated in batch experiments using MBBR carriers from polishing and nitrifying reactors. Additionally, the presence of these two metabolites in biofilm-free wastewater effluent was studied. The nitrifying biofilm reactor had a higher biological activity with k-value of 0.1813 h-1 than the reactor with polishing biofilm (k = 0.0161 h-1) which again has a much higher biological activity for removal of clindamycin than of the suspended bacteria (biofilm-free control). Clindamycin Sulfoxide was the main transformation product which was found in concentrations exceeding 10% of the initial clindamycin concentration after 1 day of MBBR treatment. Thus, MBBRs should not necessarily be considered as reactors mineralizing clindamycin as they perform transformation reactions at least to some extent.
Bioavailability of Clindamycin From a New Clindamycin Phosphate 1.2%-Benzoyl Peroxide 3% Combination Gel
Clin Pharmacol Drug Dev 2013 Jan;2(1):33-47.PMID:27121558DOI:10.1002/cpdd.7.
A new topical fixed-dose combination product containing clindamycin (1%, formulated as 1.2% clindamycin phosphate, CLNP 1.2%) with low strength (3%) benzoyl peroxide (BPO) in a methylparaben-free gel vehicle (CLNP 1.2%-BPO 3%-MPF) has been developed for the treatment of acne. The objective of this study was to determine the relative bioavailability of clindamycin and Clindamycin Sulfoxide from CLNP 1.2%-BPO 3%-MPF compared with clindamycin phosphate 1.2%-BPO 5% in a methylparaben-preserved gel vehicle (CLNP 1.2%-BPO 5%-MP) and clindamycin phosphate 1.2%-BPO 5% in a methylparaben-free gel vehicle (CLNP 1.2%-BPO 5%-MPF), and to determine whether exposure is affected by BPO concentration (3% vs. 5%) when applied topically. Seventy-two subjects with moderate-severe acne were randomized to receive CLNP 1.2%-BPO 3%-MPF, CLNP 1.2%-BPO 5%-MP, or CLNP 1.2%-BPO 5%-MPF in a 5-day, open-label, and parallel-group study. Cmax and AUC values for clindamycin were highest for CLNP 1.2%-BPO 5%-MP, followed by CLNP 1.2%-BPO 3%-MPF and CLNP 1.2%-BPO 5%-MPF, but differences were not statistically significant. Systemic exposure to clindamycin and Clindamycin Sulfoxide was low and comparable between the formulations. Results indicate that differences in BPO concentration do not influence clindamycin bioavailability.
Pharmacokinetics of clindamycin administered orally to pigeons
J Avian Med Surg 2011 Dec;25(4):259-65.PMID:22458181DOI:10.1647/2010-038.1.
To determine the plasma concentration of clindamycin in pigeons after oral administration, 12 rock pigeons (Columba livia) were used in a 2-phase study. In the first phase, 8 pigeons received clindamycin by gavage at 100 mg/kg as a single dose. Blood samples were collected at 0, 0.25, 0.5, 1, 2, 3, 4, and 6 hours, and the plasma was separated, frozen, and subsequently analyzed by liquid chromatography-mass spectrometry for clindamycin and its active metabolites, N-demethylclindamycin (NCLD) and Clindamycin Sulfoxide. Clindamycin was rapidly absorbed with plasma concentrations peaking at 0.5 hours at 1.43 microg/mL. The terminal half-life (t(1/2)) was 1.25 hours, and the mean residence time was 2.49 hours. N-demethylclindamycin was detected in 7 of 8 birds (88%), whereas Clindamycin Sulfoxide was not found in any samples. In phase 2, clindamycin was administered to 3 birds by gavage at 100 mg/ kg q6h for 5 doses. Mean peak plasma concentrations were 2.46 and 0.64 microg/mL, with trough concentrations of 0.11 and 0.44 microg/mL for clindamycin and NCLD, respectively. No adverse effects were observed in any birds. Based on an additive antimicrobial effect of NCLD with clindamycin, an oral dosage of 100 mg/kg q6h in pigeons should reach effective plasma concentrations against common susceptible pathogens. If dose proportionality exists, lower doses and longer intervals likely produce subtherapeutic concentrations to treat systemic infections. How well birds would tolerate an extended oral dose regimen, how frequently birds fail to produce the active metabolite critical for an additive effect, and the application of these results to other avian species require further study.
Clindamycin activity against chloroquine-resistant Plasmodium falciparum
J Infect Dis 1984 Dec;150(6):904-11.PMID:6389719DOI:10.1093/infdis/150.6.904.
The clindamycin dose-response curves observed with both chloroquine-resistant and chloroquine-susceptible strains of Plasmodium falciparum in vitro demonstrated a plateau region that extended from 10(-2) to 10(1) micrograms/ml of drug (22 nM to 22 microM). Similar dose-response curves were also observed with the three major metabolites of clindamycin (Clindamycin Sulfoxide, de-N-methyl clindamycin, and de-N-methyl Clindamycin Sulfoxide). The position of this plateau was time dependent and rose from 20%-25% to 90%-95% inhibition of parasite growth between 24 and 72 hr of exposure to the drug. Clinidamycin treatment reduced plasmodial protein and nucleic acid synthesis (as measured by the incorporation of [3H]isoleucine and [3H]hypoxanthine, respectively) but did not interfere with knob formation. The combination of quinine plus a fixed concentration of clindamycin (0.1 microgram/ml) inhibited growth of the quinine-resistant Indochina I strain, although most of the antiplasmodial activity observed at quinine concentrations less than 50 ng/ml (154 nM) could be attributed to clindamycin alone.