1. Anti-infection
    Cell Cycle/DNA Damage
  2. Antibiotic
    Antifolate
    Parasite
    Bacterial
  3. Trimetrexate isethionate

Trimetrexate isethionate (Synonyms: CI-898 isethionate)

Cat. No.: HY-10373B
Handling Instructions

Trimetrexate (CI-898) isethionate 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 isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.

For research use only. We do not sell to patients.

Trimetrexate isethionate Chemical Structure

Trimetrexate isethionate Chemical Structure

CAS No. : 82935-04-4

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Description

Trimetrexate (CI-898) isethionate 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 isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4].

IC50 & Target

1.35 nM (Toxoplasma gondii DHFR), 4.74 nM (human DHFR)[1]

In Vitro

Trimetrexate isethionate (0.1 μM, 18 h) completely inhibits proliferation of toxoplasma in murine macrophages[3].
Trimetrexate isethionate (1 μM) can cross the toxoplasma cell membrane and rapidly reaches high intracellular concentrations (108 pmol/107 cells within 10 min) [3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Trimetrexate (180 mg/kg or 30 mg/kg; p.o. or i.p.; daily) isethionate extends the median survival of the toxoplasma infected mice and shows antitoxoplasma activity[3]. Trimetrexate (0-30 mg/kg; i.v.; once daily for 5days) isethionate shows chronic toxicity in rats[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Toxoplasma infected female BALB/c mice weighing about 20 g[3]
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[4]
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.
Molecular Weight

495.55

Formula

C21H29N5O7S

CAS No.
SMILES

OCCS(=O)(O)=O.NC1=NC(N)=C2C(C)=C(CNC3=CC(OC)=C(OC)C(OC)=C3)C=CC2=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Trimetrexate isethionate
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