Tetroxoprim
(Synonyms: 四氧普林,HE 781) 目录号 : GC63612
Tetroxoprim 是抗菌 DHFR 的抑制剂。
Cas No.:53808-87-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tetroxoprim is an antimicrobial DHFR inhibitor[1].
Tetroxoprim brings about a 50% in vitro inhibition with E. coli, at a concentration of 4 x 10-9M[1].
[1]. H S Aschhoff, et al. Tetroxoprim--a new inhibitor of bacterial dihydrofolate reductase. J Antimicrob Chemother. 1979 Nov;5(B):19-25.
| Cas No. | 53808-87-0 | SDF | |
| 别名 | 四氧普林,HE 781 | ||
| 分子式 | C16H22N4O4 | 分子量 | 334.37 |
| 溶解度 | DMSO : 16.67 mg/mL (49.85 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light, stored under nitrogen |
| 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 | 2.9907 mL | 14.9535 mL | 29.907 mL |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 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 sulfadiazine-tetroxoprim combination (co-tetroxazine) in the treatment of the acute exacerbation of chronic bronchitis]
Minerva Med 1988 Jul;79(7):563-8.PMID:3043259doi
After considering the bacterial flora which is most common in relapses in patients with bronchitis, 40 patients with chronic bronchitis have been treated with Tetroxoprim a recently synthetized benzyl pyrimidine associated with sulfadiazine. One 350 mg tablet was administered every 12 hours for different periods, from 7 to 14 days. This study has shown how Tetroxoprim has a wide antibacterial range, how it is well tolerated and extremely powerful in treating relapses of chronic infections in bronchi.
HPLC determination of Tetroxoprim and sulphadiazine in pharmaceutical dosage forms and in biological fluids
J Pharm Biomed Anal 1989;7(1):57-65.PMID:2488608DOI:10.1016/0731-7085(89)80067-6.
Two HPLC methods for determination of Tetroxoprim and sulphadiazine in pharmaceutical dosage forms and in biological fluid are reported. Both methods show good linearity, precision, accuracy and reproducibility. The serum levels and urinary excretion of Tetroxoprim and sulphadiazine in man, after oral administration of two different syrup formulations, are reported. Tetroxoprim embonate, an insoluble salt very useful for obtaining a suspension with good palatability, shows a bioavailability not statistically different from that of Tetroxoprim base. Sulphadiazine shows the same bioavailability in the two syrups.
The pharmacokinetics of Tetroxoprim in the dog
Eur J Drug Metab Pharmacokinet 1982;7(3):197-202.PMID:7173274DOI:10.1007/BF03189566.
The pharmacokinetics and metabolism of the newly developed antibacterial Tetroxoprim (TXP) were investigated in four male beagle dogs using a 2-(14C)-labelled drug. TXP was administered intravenously and orally at doses of 5 mg/kg bodyweight. Counting of the total 14C-radioactivity shows that the drug was absorbed completely and eliminated almost exclusively by the kidneys. The quantitative absorption of TXP from the canine gastro-intestinal tract was ascertained by comparison of the AUC-values and the renal recoveries of unchanged drug following i.v. and oral dosage. The terminal half-lives of non-metabolized compound in plasma were 4.64 and 4.83 for i.v. and oral dosing respectively. Following either i.v. or oral TXP administration, the major route of excretion was renal elimination of the compound as its major metabolite U-1 (81-82.2% of dose) and as unchanged mother substance (11.4-12.3% of dose).
Bioequivalency studies on tablet formulation of Tetroxoprim and sulphadiazine
J Clin Pharm Ther 1992 Apr;17(2):97-9.PMID:1583085DOI:10.1111/j.1365-2710.1992.tb01274.x.
The paper describes a comparative bioavailability study on two tablet formulations containing 100 mg of Tetroxoprim and 250 mg of sulphadiazine. The comparison was based on the estimated pharmacokinetic parameters from time--serum concentration profiles obtained following the administration of the tablets to 12 healthy volunteers. Statistical analysis performed on the parameters showed that the differences are statistically insignificant and the formulations are bioequivalent.
Renal handling and lymph concentration of Tetroxoprim and metioprim: an experimental study in dogs
J Urol 1984 Aug;132(2):362-4.PMID:6737599DOI:10.1016/s0022-5347(17)49627-3.
The renal handling and renal lymph concentrations of Tetroxoprim and metioprim, 2 trimethoprim analogs, were investigated during constant intravenous infusion in 8 dogs. The mean ratios of Tetroxoprim and metioprim clearance to creatinine clearance were 0.40 and 0.16 respectively. After compensation for protein binding, both antimicrobials were found to undergo a renal tubular net reabsorption of 55 to 60 per cent of the filtered amount. Renal lymph was obtained by direct cannulation of capsular lymphatics, and the mean lymph-to-arterial plasma concentration ratios were 0.93 and 0.74 for Tetroxoprim and metioprim, respectively. Renal tissue concentrations of the 2 microbials were many times higher than the simultaneous concentrations in plasma, suggesting that lymph concentrations do not represent the entire interstitial compartment or that significant amounts of antimicrobial are located intracellularly. Tetroxoprim and metioprim concentrated well in the kidney, but their potential use in the treatment of pyelonephritis awaits verification in clinical trials.