S85635 |
Trimetrexate |
源叶(MedMol) | 98% |
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- 产品描述: Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer
- 靶点: Toxoplasma
- 体内研究:
Trimetrexate (180 mg/kg or 30 mg/kg; p.o. or i.p.; daily) extends the median survival of the toxoplasma infected mice and shows antitoxoplasma activity. Trimetrexate (0-30 mg/kg; i.v.; once daily for 5days) shows chronic toxicity in rats Animal Model: Toxoplasma infected female BALB/c mice weighing about 20 g Dosage: 180 mg/kg or 30 mg/kg Administration: 180 mg/kg per day orally in the drinking water or 30 mg/kg per day i.p. Result: Extended the median survival of the infected mice to 10 d (p.o.) or 19 d (i.p.).
- 参考文献:
1. Hopper AT, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019 Feb 14;62(3):1562-1576. 2. Fulton, B., et al. Trimetrexate. Drugs 49, 563–576 (1995). 3. Allegra CJ, et al. Potent in vitro and in vivo antitoxoplasma activity of the lipid-soluble antifolate trimetrexate. J Clin Invest. 1987 Feb;79(2):478-82. 4. Dethloff LA, et al. Chronic toxicity of the anticancer agent trimetrexate in rats. Fundam Appl Toxicol. 1992 Jul;19(1):6-14. 5. Grem JL, Voeller DM, Geoffroy F, Horak E, Johnston PG, Allegra CJ. Determinants of trimetrexate lethality in human colon cancer cells. Br J Cancer. 1994 Dec;70(6):1075-84.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.707 ml 13.535 ml 27.069 ml 5 mM 0.541 ml 2.707 ml 5.414 ml 10 mM 0.271 ml 1.353 ml 2.707 ml 50 mM 0.054 ml 0.271 ml 0.541 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)