Trimethoprim lactate

SKU: orb2900934

Description

Trimethoprim lactate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim lactate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 23256-42-0
• MW: 380.401
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₄N₄O₆
• SMILES: C[C@H](O)C(O)=O.COc1cc(Cc2cnc(N)nc2N)cc(OC)c1OC
• Solubility: In Vitro: DMSO : 250 mg/mL (657.20 mM; Ultrasonic )H2O : 16.67 mg/mL (43.82 mM; Ultrasonic)

Bioactivity

• 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. 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).
• 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.

Storage & Handling

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