Trimetrexate glucuronate_product_DataBase

Bioactivity	Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia[1][2].
Invitro	Trimetrexate glucuronate (0.05-1 μM 6 h) results in a decrease in adenosine and guanosine acids and a significant increase in the pyrimidine nucleotide such as CTP, UTP of WI-L2 human lymphoblastoid cells in a dose-dependent manner[1].Trimetrexate glucuronate (1 μM, 2 h) can reduce the level of dTTP by 29%, also decrease in the dGTP and dATP, while cause extensive inhibition of deoxyuridine incorporation into DNA in L1210 mouse leukemia cells[1].
In Vivo	Trimetrexate glucuronate (i.p., 100-225 mg/kg, daily, day 1, 5, 9) has antitumor activity in inbred DBA/2 mice with L1210 leukemia[1]. Animal Model:
Name	Trimetrexate glucuronate
CAS	82952-64-5
Formula	C25H33N5O10
Molar Mass	563.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. R C Jackson, et al. Biochemical pharmacology of the lipophilic antifolate, trimetrexate. Adv Enzyme Regul. 1984;22:187-206. [2]. P J Harris, et al. Trimetrexate glucuronate associated with anti-Kaposi sarcoma effect. AIDS Patient Care STDS. 1996 Oct;10(5):280-1.

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