产品
编 号：F377817
分子式：C19H23N5O3
分子量：369.42
分子式：C19H23N5O3
分子量：369.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 52128-35-5
产品详情
生物活性：
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.
体内研究：
Trimetrexate (180 mg/kg 或 30 mg/kg；po 或腹腔注射；每天) 可延长弓形虫感染小鼠的中位生存期，并显示出抗弓形虫活性。Trimetrexate (0-30 mg/kg；iv；每天一次，持续 5 天) 在大鼠中表现出慢性毒性。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.).
Animal Model:Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g
Dosage:0, 1, 10, or 30 mg/kg
Administration:Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period
Result:Showed chronic toxicity, the testicular changes persisting during the course of multiple cycles of dosing were not reversible within 21 days, but required an additional 56 days for essentially complete recovery.
体外研究：
Trimetrexate (0.1 μM，18 h) 完全抑制小鼠巨噬细胞中弓形虫的增殖。 Trimetrexate (1 μM) 可穿过弓形虫细胞膜并迅速达到细胞内高浓度 (108 pmol/107 个细胞，10 分钟内)。 Trimetrexate (0.1 mM；24 小时) 在 SNU-中抑制细胞生长 50-60% C4 和 NCI-H630 细胞系。 Trimetrexate (1 和 10 mM；24 小时) 在 C4 细胞中产生致死性并抑制 DHFR。
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.
体内研究：
Trimetrexate (180 mg/kg 或 30 mg/kg；po 或腹腔注射；每天) 可延长弓形虫感染小鼠的中位生存期，并显示出抗弓形虫活性。Trimetrexate (0-30 mg/kg；iv；每天一次，持续 5 天) 在大鼠中表现出慢性毒性。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.).
Animal Model:Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g
Dosage:0, 1, 10, or 30 mg/kg
Administration:Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period
Result:Showed chronic toxicity, the testicular changes persisting during the course of multiple cycles of dosing were not reversible within 21 days, but required an additional 56 days for essentially complete recovery.
体外研究：
Trimetrexate (0.1 μM，18 h) 完全抑制小鼠巨噬细胞中弓形虫的增殖。 Trimetrexate (1 μM) 可穿过弓形虫细胞膜并迅速达到细胞内高浓度 (108 pmol/107 个细胞，10 分钟内)。 Trimetrexate (0.1 mM；24 小时) 在 SNU-中抑制细胞生长 50-60% C4 和 NCI-H630 细胞系。 Trimetrexate (1 和 10 mM；24 小时) 在 C4 细胞中产生致死性并抑制 DHFR。
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