Trimethoprim

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Trimethoprim 是一种二氢叶酸还原酶抑制剂抗菌剂。

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.

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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).

NIH 204 | NSC 106568

Cell Cycle/DNA Damage

DHFR

DHFR| Thymidylate synthase

Inflammation/Immunology

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738-70-5

290.32

C14H18N4O3

>98% (HPLC)

DMSO: 58 mg/mL (199.77 mM)

NC1=NC=C(CC2=CC(OC)=C(OC)C(OC)=C2)C(N)=N1

5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine

(-20℃)

With Ice Pack

≥ 2 years