[CAS NO. 23256-42-0] Trimethoprim lactate

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PRODUCTS SPECIFICATIONS [23256-42-0]

Catalog

HY-B0510C

Brand

MCE

CAS

23256-42-0

DESCRIPTION [23256-42-0]

Overview

MDL	MFCD00171722
Molecular Weight	380.40
Molecular Formula	C17H24N4O6
SMILES	CC(O)C(O)=O.NC1=NC=C(CC2=CC(OC)=C(OC)C(OC)=C2)C(N)=N1

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

3 Publications Citing Use of MCE

Summary

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 ^[1] ^[2] ^[3] ^[4] .

IC50 & Target

Dihydrofolate reductase, Bacteria ^[1]
Influenza A virus ^[4]

In Vitro

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.

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 ^[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).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00752375	University of Alberta\|Canadian Urological Association	Pyelonephritis	February 2009	Phase 3
NCT02879981	Hoffmann-La Roche	Bronchitis	November 10, 2016
NCT01137903	Universidad Complutense de Madrid	Osteomyelitis\|Diabetic Foot\|Diabetic Foot Ulcers	April 2010	Not Applicable
NCT00869518	University of California, San Francisco	Staphylococcus Aureus\|HIV Infections	July 2009	Phase 2
NCT02902640	Hoffmann-La Roche	Bronchitis	November 15, 2016
NCT00078559	University of Wisconsin, Madison\|Immune Tolerance Network (ITN)	Kidney Transplantation\|Kidney Disease	November 2003	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
NCT00002002	Lederle Laboratories\|NIH AIDS Clinical Trials Information Service	Pneumonia, Pneumocystis Carinii\|HIV Infections		Not Applicable
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
NCT00002120	U.S. Bioscience\|Jacobus Pharmaceutical\|NIH AIDS Clinical Trials Information Service	Pneumonia, Pneumocystis Carinii\|HIV Infections		Phase 1
NCT01140516	McMaster University\|The Physicians´ Services Incorporated Foundation\|Hamilton Health Sciences Corporation\|McMaster Surgical Associates	Hydronephrosis\|Urinary Tract Infection	July 2010	Not Applicable
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
NCT03919435	University of Pennsylvania	Granulomatosis With Polyangiitis\|Wegener Granulomatosis	March 27, 2019	Phase 1\|Phase 2
NCT00002850	Gary Morrow\|National Cancer Institute (NCI)\|Eastern Cooperative Oncology Group\|University of Rochester	Infection\|Multiple Myeloma	March 1997	Phase 3
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
NCT00380640	The Hospital for Sick Children	Epidermolysis Bullosa	September 2006	Phase 2
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
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
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
NCT02371603	GlaxoSmithKline	Anaemia	February 11, 2015	Phase 1
NCT03077711	NorthShore University HealthSystem	Urinary Tract Infections, Recurrent	June 2016	Phase 4
NCT05418777	William Beaumont Hospitals	COPD Exacerbation Acute	September 28, 2022	Phase 1\|Phase 2
NCT05398679	Fundacion Clinic per a la Recerca Biomédica	Endocarditis Infective	June 1, 2022	Phase 4
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
NCT01757236	University Hospital, Tours\|Pfizer\|International Clinical Trials Association	Hip Prosthetic Joint Infection	October 2012	Phase 2
NCT00002283	Jacobus Pharmaceutical\|NIH AIDS Clinical Trials Information Service	Pneumonia, Pneumocystis Carinii\|HIV Infections		Not Applicable
NCT05268120	Leiden University Medical Center	MRSA	July 25, 2022	Not Applicable
NCT04306731	University of Sulaimani	Recurrent Urinary Tract Infection	September 20, 2014	Not Applicable
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
NCT01507974	HaEmek Medical Center, Israel	Pregnancy Complications	January 16, 2012	Not Applicable
NCT05274672	Baylor Research Institute\|Albert Einstein Healthcare Network	Benign Prostatic Hyperplasia\|Urinary Tract Infections	March 1, 2022	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 657.20 mM ; Need ultrasonic)

H ₂ O : 16.67 mg/mL ( 43.82 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6288 mL	13.1441 mL	26.2881 mL
5 mM	0.5258 mL	2.6288 mL	5.2576 mL
10 mM	0.2629 mL	1.3144 mL	2.6288 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution
4.

Add each solvent one by one: PBS

Solubility: 2 mg/mL (5.26 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

* All of the co-solvents are available by MCE.

References

Synonyms

Propanoic acid, 2-hydroxy-, compd. with 5-[(3,4,5-trimethoxyphenyl)methyl]-2,4-pyrimidinediamine (1:1)

Lactic acid, compd. with 2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine (1:1)

2,4-Pyrimidinediamine, 5-[(3,4,5-trimethoxyphenyl)methyl]-, mono(2-hydroxypropanoate)

Trimethoprim lactate

Lactotrim

2,4-Diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine lactate