Trimethoprim

SKU: orb1224102

Description

Trimethoprim is a Dihydrofolate Reductase Inhibitor Antibacterial.(In Vitro):Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF).Trimethoprim (3 μg/mL; 1 h) induces protein aggregation and main heat shock proteins (Hsps) in E. coli cells, which indicates that Trimethoprim sulfate presence leads to protein misfolding.Trimethoprim (1.5-3 μg/mL; 1 h) causes induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps in E. coli cells exposed to folate and heat stress.(In Vivo):Trimethoprim (10 mg/kg; i.v.; once every 12 h; 3 d) shows antibacterial activity against H. influenzae, S. pneumoniae, E. coli and N. meningitidis in infected mice.Trimethoprim can be connected with the thiomaltose (TM-TMP) and shows stability with a half-life of about 1 hour in complete serum, and has an MIC value around 1 μM against E. coli.Trimethoprim (10 mg/mL; 0.5 mL; inject with Trimethoprim-Zn combined suspension) decreases the virus titer and increases the survival rate of chicken embryo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 738-70-5
• MW: 290.32
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₈N₄O₃
• SMILES: NC1=NC=C(CC2=CC(OC)=C(OC)C(OC)=C2)C(N)=N1
• Target: DHFR
• Solubility: DMSO: 58 mg/mL (199.77 mM)

Bioactivity

• In Vivo:
  Animal model: Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×107 CFU of E. coli under 3% isoflurane). Dosage: 10 mg/kg. Administration: i. v. ; once every 12 h; for 3 d. Result: Showed antibacterial activity against H. influenzae, S. pneumoniae, E. coli and N. meningitidis with CD50s of 150 mg/kg, 335 mg/kg, 27.5 mg/kg and 8.4 mg/kg, respectively in infected mice. Animal model: Fertilized eggs (injected H3N2 virus into amniotic and allantoic space at day 8). Dosage: 10 mg/mL; 0.5 mL. Administration: The Trimethoprim-Zn combined suspension was injected into the air sac; single dosage. Result: Decreased the virus titer and increased the survival rate of chicken embryo. The survival rate peaked at ratio about 0.18 (Zn/Trimethoprim).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NIH 204 | NSC 106568

Quick Database Links

Gene Symbol

DHFR