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Trimethoprim lactate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Trimethoprim lactate图片
CAS NO:23256-42-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
500mg电议
1 g电议
5 g电议

产品名称
乳酸甲氧苄啶
产品介绍
Trimethoprim lactate 是一种抑菌抗生素 (antibiotic),也是一种具有口服活性的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂。Trimethoprim lactate 对多种革兰氏阳性 (Gram-positive) 和革兰氏阴性需氧细菌 (Gram-negative aerobic bacteria) 具有活性。Trimethoprim lactate 可用于尿路感染,志贺氏菌病和肺孢子菌肺炎的研究。Trimethoprim lactate 与锌联合使用可抑制甲型流感病毒 (Influenza A virus) 对鸡胚的感染。
生物活性

Trimethoprim lactate is a bacteriostaticantibioticand an orally activedihydrofolate reductaseinhibitor. Trimethoprim lactate is active against a wide range ofGram-positiveandGram-negative aerobic bacteria. Trimethoprim lactate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim lactate can inhibitinfectionofInfluenza A virusin chick embryo when combinated with zinc[1][2][3][4].

IC50& Target

Dihydrofolate reductase, Bacteria[1]
Influenza A virus[4]

体外研究
(In Vitro)

Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF)[1].
Trimethoprim (3 μg/mL; 1 h) induces protein aggregation and main heat shock proteins (Hsps) in E. coli cells, which indicates that Trimethoprim sulfate presence leads to protein misfolding[1].
Trimethoprim (1.5-3 μg/mL; 1 h) causes induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps inE. colicells exposed to folate and heat stress[1].

体内研究
(In Vivo)

Trimethoprim (10 mg/kg; i.v.; once every 12 h; 3 d) shows antibacterial activity againstH. influenzae,S. pneumoniae,E. coliandN. meningitidisin infected mice[2].
Trimethoprim can be connected with the thiomaltose (TM-TMP) and shows stability with a half-life of about 1 hour in complete serum, and has an MIC value around 1 μM againstE. coli[2].
Trimethoprim (10 mg/mL; 0.5 mL; inject with Trimethoprim-Zn combined suspension) decreases the virus titer and increases the survival rate of chicken embryo[4].

Animal Model:Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×107CFU ofE. coliunder 3% isoflurane)[2]
Dosage:10 mg/kg
Administration:i.v.; once every 12 h; for 3 d
Result:Showed antibacterial activity againstH. influenzae,S. pneumoniae,E. coliandN. meningitidiswith CD50s of 150 mg/kg, 335 mg/kg, 27.5 mg/kg and 8.4 mg/kg, respectively in infected mice.
Animal Model:Fertilized eggs (injected H3N2 virus into amniotic and allantoic space at day 8)[4]
Dosage:10 mg/mL; 0.5 mL
Administration:The Trimethoprim-Zn combined suspension was injected into the air sac; single dosage
Result:Decreased the virus titer and increased the survival rate of chicken embryo.
The survival rate peaked at ratio about 0.18 (Zn/Trimethoprim).
Clinical Trial
分子量

380.40

性状

Solid

Formula

C17H24N4O6

CAS 号

23256-42-0

中文名称

乳酸甲氧苄啶; 乳酸甲氧苄氨嘧啶; 乳酸甲氧苄嘧啶; 乳酸甲氧苄胺嘧啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL(657.20 mM;Need ultrasonic)

H2O : 16.67 mg/mL(43.82 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6288 mL13.1441 mL26.2881 mL
5 mM0.5258 mL2.6288 mL5.2576 mL
10 mM0.2629 mL1.3144 mL2.6288 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.47 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 4.

    请依序添加每种溶剂: PBS

    Solubility: 2 mg/mL (5.26 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。