Cinoxacin (Compound 64716)
(Synonyms: 西诺沙星; Compound 64716) 目录号 : GC34054
Cinoxacin (Compound 64716) (Compound 64716)，一种与喹诺酮类口服活性抗菌剂相关的合成抗菌剂。
Cas No.:28657-80-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics, with activity similar to oxolinic acid and nalidixic acid.
| Cas No. | 28657-80-9 | SDF | |
| 别名 | 西诺沙星; Compound 64716 | ||
| Canonical SMILES | O=C(C1=NN(CC)C2=C(C=C3C(OCO3)=C2)C1=O)O | ||
| 分子式 | C12H10N2O5 | 分子量 | 262.22 |
| 溶解度 | DMSO : 18.66 mg/mL (71.16 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 | 3.8136 mL | 19.068 mL | 38.1359 mL |
| 5 mM | 0.7627 mL | 3.8136 mL | 7.6272 mL |
| 10 mM | 0.3814 mL | 1.9068 mL | 3.8136 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。
Cinoxacin: in vitro antibacterial studies of a new synthetic organic acid
Antimicrob Agents Chemother 1975 Feb;7(2):159-63.PMID:1094949DOI:10.1128/AAC.7.2.159.
Cinoxacin (Compound 64716) is a synthetic organic acid with antibacterial activity against most aerobic gram-negative bacilli. Minimal inhibitory concentrations of cinoxacin (agar-dilution method) were determined for 419 strains. Escherichia coli was the most susceptible group of organisms. The majority of Klebsiella sp., Enterobacter sp., Proteus sp., and Serratia marcescens were inhibited by 8 mug of cinoxacin per ml. Pseudomonas aeruginosa and all gram-positive isolates tested were resistant to 64 mug or less of cinoxacin per ml. Zones of inhibition using a 30-mug disk correlated well with agar-dilution minimal inhibitory concentrations (r = -0.9). Cinoxacin was bactericidal when tested with inocula of 5 x 10(6) organisms per ml. Resistance to cinoxacin was readily developed in all three strains tested by serial passage on drug-containing agar. The in vitro properties of this agent were similar to those of nalidixic acid.
Cinoxacin (Cinobac, Eli Lilly & Co.)
Drug Intell Clin Pharm 1982 Dec;16(12):916-21.PMID:6759090DOI:10.1177/106002808201601203.
Cinoxacin, a synthetic organic acid antibacterial agent, related structurally to nalidixic and oxolinic acid, has been approved for the treatment of initial and recurrent urinary tract infections (UTIs) caused by susceptible gram-negative microorganisms. The role of Cinoxacin in the treatment of UTIs, compared with the usual first-line agents, is uncertain at this time. The efficacy of Cinoxacin in the treatment of pyelonephritis, compared with these proven agents, has been examined in only small numbers of patients, and Cinoxacin is more expensive than these agents. Cinoxacin may prove valuable in the treatment of prostatitis and in the prophylaxis of recurrent UTIs; further study in these areas is warranted. In the routine treatment of acute UTIs, Cinoxacin perhaps should be reserved only for those patients with organisms resistant to usual first-line agents or those who fail to respond to therapy with these agents. In this respect, Cinoxacin may, in the future, replace nalidixic acid.
Cinoxacin: effectiveness against experimental pyelonephritis in rats
Antimicrob Agents Chemother 1974 Oct;6(4):432-6.PMID:4157340DOI:10.1128/AAC.6.4.432.
The antimicrobial activity of Cinoxacin, 1-ethyl-4(1H)-oxo-[1,3]dioxolo[4,5-g]cinnoline-3-carboxylic acid, previously reported as Compound 64716, was determined and compared with other antimicrobial agents at a dosage of 12 mg/kg once daily in a descending pyelonephritis rat model with Escherichia coli and Proteus mirabilis as infecting organisms. Cinoxacin was considerably more effective than either nalidixic acid or oxolinic acid when all three were administered orally at 3 mg/kg four times daily. The presence of demonstrable serum activity with a high recovery in urine indicates Cinoxacin possesses highly desirable properties of an effective oral chemotherapeutic agent for urinary tract infections.
Time-dependent elimination of Cinoxacin in rats
J Pharm Sci 1984 Dec;73(12):1697-700.PMID:6527237DOI:10.1002/jps.2600731208.
The effect of the variation of urinary pH on the pharmacokinetics of the acidic antibacterial agent, Cinoxacin (pKa 4.60), was examined. Urinary pH of 24-h fasted rats remained at about pH 6 during the daytime, while that of nonfasted rats was high (about pH 7.5) in the morning and gradually decreased to a pH similar to that of the fasted rat in the afternoon. The free fraction of Cinoxacin in fasted rat sera in the morning was similar to that in nonfasted rats despite the longer half-life of Cinoxacin in fasted rats. In the afternoon the free fraction was slightly different despite similar Cinoxacin elimination in fasted and nonfasted rats. These findings seemed to exclude the contribution of protein binding from the causes of increased Cinoxacin elimination in nonfasted rats in the morning. Elimination rate constants of Cinoxacin obtained with a one-compartment open model correlated well with urinary pH 30 min after injection, suggesting that the urinary pH plays a more important role in Cinoxacin elimination. When Cinoxacin was orally administered to fasted rats at 11:00, the area under the plasma concentration-time curve was threefold larger than in nonfasted rats. As found with the intravenous administration, this difference may be explained by the prolonged half-life caused by decreased urinary pH after fasting. This study revealed the time-dependent elimination of Cinoxacin in nonfasted rats, which is related to physiological change of urinary pH caused by food intake.
Influence of urinary pH on the pharmacokinetics of Cinoxacin in humans and on antibacterial activity in vitro
Antimicrob Agents Chemother 1982 Mar;21(3):472-80.PMID:7103450DOI:10.1128/AAC.21.3.472.
The impact of acidification and alkalinization of the urine on the pharmacokinetics of Cinoxacin was examined after single 500-mg oral doses were administered to nine healthy male volunteers. Acidic and alkaline conditions were achieved by repeated oral doses of ammonium chloride or sodium bicarbonate, respectively. Plasma Cinoxacin levels in all subjects were adequately described in terms of one-compartment-model kinetics with first-order absorption and elimination. Acidification and alkalinization treatment had no effect on Cinoxacin absorption or distribution. The mean elimination half-life of Cinoxacin in plasma was 1.1, 2.0, and 0.6 h in control subjects and with acidification and alkalinization of urine, respectively. Recovery of intact Cinoxacin in samples of urine collected 0 to 36 h after Cinoxacin administration represented 65% of the dose in control subjects and urine acidification and 80% of the dose with alkalinization of urine. The mean renal clearance of Cinoxacin was 76, 118, and 278 ml/min with acidification, control, and alkalinization, respectively, and renal clearance was highly correlated with urinary pH. Urine concentrations of Cinoxacin were significantly higher with alkalinization compared with control values during the first 4 h after drug administration. Urine Cinoxacin concentrations were reduced somewhat by acidification, but these tended not to be significantly different from control values. Changes in Cinoxacin elimination owing to urine pH are less pronounced in humans than in dogs. The antibacterial activity of Cinoxacin against some common urinary tract pathogens was pH dependent. A four- to eightfold reduction in Cinoxacin activity was generally observed at pH 8 compared with lower pH values. However, in view of the high levels of Cinoxacin which are obtained in both acidic and basic urine, the impact of urine pH on Cinoxacin antibacterial efficacy would be of minor clinical importance.