| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1g |
|
||
| 5g |
|
||
| 10g |
|
||
| 25g |
|
||
| 50g |
|
||
| 100g |
|
||
| 200g |
|
||
| Other Sizes |
|
| 体外研究 (In Vitro) |
通过阻止二氢叶酸 (DHFR) 将二氢叶酸转化为四氢叶酸 (THF)，甲氧苄啶可防止身体获得叶酸支持 [1]。在大肠杆菌中，甲氧苄啶（3 μg/mL；1 小时）会导致显着的热休克蛋白 (Hsps) 和蛋白质聚集。大肠杆菌细胞，表明蛋白质错误折叠是由硫酸甲氧苄啶引起的[1]。诱导大肠杆菌的 DnaK、DnaJ、GroEL、ClpB 和 IbpA/B Hsp（1.5–3 μg/mL；1 小时）。大肠杆菌，并且受刺激的细胞受到热量和叶酸的作用[1]。
|
|---|---|
| 体内研究 (In Vivo) |
甲氧苄氨嘧啶（10 mg/kg；静脉注射；每 12 小时；3 天）表现出对幽门螺杆菌的抗菌活性。对脑膜炎球菌感染、肺炎链球菌、流感细菌等具有保护作用 [2]。它可以与硫代麦芽糖 (TM-TMP) 结合并表现出稳定性，在完全血清中的半衰期约为 1 小时，针对大肠杆菌的 MIC 值约为 1 微克 [2]。
|
| 动物实验 |
Animal/Disease Models: Female C3H/HeOuJ mouse (transurethral infection containing 1-2 × 107 in 50 μL suspension of 3% E. coli CFU in isoflurane) [2]
Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection; once every 12 hrs (hrs (hours)); 3 d Experimental Results: It has antibacterial activity against Haemophilus influenzae, Streptococcus pneumoniae, Escherichia coli and Neisseria meningitidis. The CD50 of infected patients is 150 mg respectively. /kg, 335 mg/kg, 27.5 mg/kg and 8.4 mg/kg mice. Animal/Disease Models: Fertilized eggs (H3N2 virus is injected into the amniotic membrane and allantoic cavity on day 8) [4] Doses: 10 mg/mL; 0.5 mL Route of Administration: Trimethoprim-zinc composite suspension is injected into the air sac; single dose Experimental Results: The virus titer was diminished and the survival rate of chicken embryos was improved. Survival rates peaked at a ratio of approximately 0.18 (Zn/trimethoprim). |
| 参考文献 |
[1]. Laskowska, E., et al., Trimethoprim induces heat shock proteins and protein aggregation in E. coli cells. Curr Microbiol, 2003. 47(4): p. 286-9.
[2]. Brogden, R.N., et al., Trimethoprim: a review of its antibacterial activity, pharmacokinetics and therapeutic use in urinary tract infections. Drugs, 1982. 23(6): p. 405-30. [3]. Xiaojian Wang, et al. A Trimethoprim Conjugate of Thiomaltose Has Enhanced Antibacterial Efficacy In Vivo. Bioconjug Chem. 2018 May 16;29(5):1729-1735. [4]. El Habbal MH. Combination therapy of zinc and trimethoprim inhibits infection of influenza A virus in chick embryo. Virol J. 2021 Jun 3;18(1):113. |
| 分子式 |
C14H18N4O3
|
|---|---|
| 分子量 |
290.32
|
| CAS号 |
738-70-5
|
| 相关CAS号 |
Trimethoprim lactate;23256-42-0;Trimethoprim-d9;1189460-62-5;Trimethoprim-d3;1189923-38-3;Trimethoprim sulfate;56585-33-2;Trimethoprim hydrochloride;60834-30-2;Trimethoprim-13C3;1189970-95-3
|
| SMILES |
NC1=NC=C(CC2=CC(OC)=C(OC)C(OC)=C2)C(N)=N1
|
| InChi Key |
IEDVJHCEMCRBQM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H18N4O3/c1-19-10-5-8(6-11(20-2)12(10)21-3)4-9-7-17-14(16)18-13(9)15/h5-7H,4H2,1-3H3,(H4,15,16,17,18)
|
| 化学名 |
5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine
|
| 别名 |
Proloprim; Trimethoprim; Trimpex, Monotrim, Triprim among others
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外) |
DMSO : ~50 mg/mL (~172.22 mM)
H2O : ~0.67 mg/mL (~2.31 mM) |
|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4445 mL | 17.2224 mL | 34.4448 mL | |
| 5 mM | 0.6889 mL | 3.4445 mL | 6.8890 mL | |
| 10 mM | 0.3444 mL | 1.7222 mL | 3.4445 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
DK-507K
Combi-2
TLN-58
Piscidin-1 (22-42)
InvivoChem的所有产品仅用于作科学研究，不面向患者销售
Copyright 2020 InvivoChem LLC | All Rights Reserved 粤ICP备20063088号-1
COA
粤公网安备 44011102003439号