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Catalog: | HY-B0510 |
Brand: | MCE |
CAS: | 738-70-5 |
MDL | MFCD00036761 |
---|---|
Molecular Weight | 290.32 |
Molecular Formula | C14H18N4O3 |
SMILES | NC1=NC=C(CC2=CC(OC)=C(OC)C(OC)=C2)C(N)=N1 |
Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria . Trimethoprim has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim can inhibit infection of Influenza A virus in chick embryo when combinated with zinc [1] [2] [3] [4] .
Trimethoprim interrupts folate metabolism by inhibition of the activity of dihydrofolase reductase (DHFR), which reduces dihydrofolate to tetrahydrofolate (THF)
[1]
.
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
[1]
.
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
[2]
.
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
[2]
.
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
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Female C3H/HeOuJ mice (transurethrally infected with a 50 μL suspension containing 1-2×10 7 CFU of E. coli under 3% isoflurane) [2] |
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 CD 50 s 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) [4] |
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). |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT01757236 | University Hospital, Tours|Pfizer|International Clinical Trials Association |
Hip Prosthetic Joint Infection
|
October 2012 | Phase 2 |
NCT00869518 | University of California, San Francisco |
Staphylococcus Aureus|HIV Infections
|
July 2009 | Phase 2 |
NCT02188472 | Henrik Enghusen Poulsen|Klinisk Biokemisk Afdeling|Klinisk farmakologisk Afdeling|Sektion for Biomedicin Institut for Veterinær Patobiologi|Rigshospitalet, Denmark |
Oxidative Stress
|
November 2010 | Phase 1 |
NCT00002002 | Lederle Laboratories|NIH AIDS Clinical Trials Information Service |
Pneumonia, Pneumocystis Carinii|HIV Infections
|
Not Applicable | |
NCT00002283 | Jacobus Pharmaceutical|NIH AIDS Clinical Trials Information Service |
Pneumonia, Pneumocystis Carinii|HIV Infections
|
Not Applicable | |
NCT02371603 | GlaxoSmithKline |
Anaemia
|
February 11, 2015 | Phase 1 |
NCT00141037 | National Institute of Allergy and Infectious Diseases (NIAID)|Astellas Pharma Inc|Hoffmann-La Roche |
Kidney Diseases|Kidney Transplantation|Kidney Transplant|Renal Transplantation|Renal Transplant
|
March 2004 | Phase 1|Phase 2 |
NCT00014911 | National Institute of Allergy and Infectious Diseases (NIAID)|Immune Tolerance Network (ITN) |
Diabetes Mellitus, Insulin-Dependent
|
April 2001 | Phase 2 |
NCT03077711 | NorthShore University HealthSystem |
Urinary Tract Infections, Recurrent
|
June 2016 | Phase 4 |
NCT05268120 | Leiden University Medical Center |
MRSA
|
July 25, 2022 | Not Applicable |
NCT00078559 | University of Wisconsin, Madison|Immune Tolerance Network (ITN) |
Kidney Transplantation|Kidney Disease
|
November 2003 | Phase 1|Phase 2 |
NCT03489629 | University of North Carolina, Chapel Hill|University of Washington|Cook Children´s Medical Center|Indiana University|University of Michigan|University of Texas Southwestern Medical Center|St. Louis Children´s Hospital |
Cystic Fibrosis
|
April 3, 2018 | Phase 2 |
NCT02879981 | Hoffmann-La Roche |
Bronchitis
|
November 10, 2016 | |
NCT03746106 | University of California, San Francisco|Tufts University|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|University of California, Davis |
Vitamin B1 Deficiency|Thiamine Deficiency
|
January 28, 2019 | Phase 4 |
NCT01820897 | JOSE MANUEL ARREOLA GUERRA|Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran |
Urinary Tract Infection|Asymptomatic Bacteriuria|Allograft Rejection|Microbiologic Resistance|Hospitalization
|
April 2013 | Phase 4 |
NCT04306731 | University of Sulaimani |
Recurrent Urinary Tract Infection
|
September 20, 2014 | Not Applicable |
NCT00380640 | The Hospital for Sick Children |
Epidermolysis Bullosa
|
September 2006 | Phase 2 |
NCT05418777 | William Beaumont Hospitals |
COPD Exacerbation Acute
|
September 28, 2022 | Phase 1|Phase 2 |
NCT00752375 | University of Alberta|Canadian Urological Association |
Pyelonephritis
|
February 2009 | Phase 3 |
NCT05398679 | Fundacion Clinic per a la Recerca Biomédica |
Endocarditis Infective
|
June 1, 2022 | Phase 4 |
NCT05274672 | Baylor Research Institute|Albert Einstein Healthcare Network |
Benign Prostatic Hyperplasia|Urinary Tract Infections
|
March 1, 2022 | Phase 4 |
NCT01137903 | Universidad Complutense de Madrid |
Osteomyelitis|Diabetic Foot|Diabetic Foot Ulcers
|
April 2010 | Not Applicable |
NCT03173053 | Radboud University Medical Center|ZonMw: The Netherlands Organisation for Health Research and Development|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|University College, London |
Staphylococcus Aureus|Motility Disorder
|
February 8, 2018 | Not Applicable |
NCT01140516 | McMaster University|The Physicians´ Services Incorporated Foundation|Hamilton Health Sciences Corporation|McMaster Surgical Associates |
Hydronephrosis|Urinary Tract Infection
|
July 2010 | Not Applicable |
NCT02902640 | Hoffmann-La Roche |
Bronchitis
|
November 15, 2016 | |
NCT00002120 | U.S. Bioscience|Jacobus Pharmaceutical|NIH AIDS Clinical Trials Information Service |
Pneumonia, Pneumocystis Carinii|HIV Infections
|
Phase 1 | |
NCT03235947 | Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Laboratorios Senosiain, S.A. de C.V. |
Urinary Tract Infection|Asymptomatic Bacteriuria
|
September 7, 2016 | Phase 4 |
NCT00002850 | Gary Morrow|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group|University of Rochester |
Infection|Multiple Myeloma
|
March 1997 | Phase 3 |
NCT03919435 | University of Pennsylvania |
Granulomatosis With Polyangiitis|Wegener Granulomatosis
|
March 27, 2019 | Phase 1|Phase 2 |
NCT01507974 | HaEmek Medical Center, Israel |
Pregnancy Complications
|
January 16, 2012 | Not Applicable |
NCT02145338 | Newcastle-upon-Tyne Hospitals NHS Trust|NHS Health Technology Assessment Programme|Newcastle University|Glasgow Caledonian University|University of Aberdeen|Cambridge University Hospitals NHS Foundation Trust|North Bristol NHS Trust|University of Southampton |
Urinary Tract Infections, Recurrent
|
September 2013 | Phase 4 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 50 mg/mL ( 172.22 mM ; Need ultrasonic)
H 2 O : 0.67 mg/mL ( 2.31 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.4445 mL | 17.2224 mL | 34.4447 mL |
5 mM | 0.6889 mL | 3.4445 mL | 6.8889 mL |
10 mM | 0.3444 mL | 1.7222 mL | 3.4445 mL |
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