CAS 56066-63-8|Aditoprime

Introduction:Basic information about CAS 56066-63-8|Aditoprime, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAditoprime
CAS Number56066-63-8Molecular Weight303.36000
Density1.233g/cm3Boiling Point503.9ºC at 760 mmHg
Molecular FormulaC15H21N5O2Melting Point/
MSDS/Flash Point258.5ºC

Names

Name5-[[4-(dimethylamino)-3,5-dimethoxyphenyl]methyl]pyrimidine-2,4-diamine
SynonymMore Synonyms

Aditoprime BiologicalActivity

DescriptionAditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics[1][2][3].
Related CatalogResearch Areas >>InfectionSignaling Pathways >>Cell Cycle/DNA Damage >>AntifolateSignaling Pathways >>Anti-infection >>Bacterial
In VitroAditoprime has the same antibacterial spectrum as TMP. Salmonellaand Streptococcus from swine, E. coli and Salmonella from chickens, E. coli, Streptococcus, Mannheimia, and Pasteurella from calves, Streptococcus and Mannheimia from sheep, and E. coli, Flavobacterium columnare, A. baumannii and Y. ruckeri from fishes are highly susceptible to Aditoprime (MIC or MIC50 ≤ 4 μg/mL)[1].
In VivoAditoprime (Aditoprim) has longer elimination half-lives (3.3~14.8 h) and higher distribution volumes (4.6~10.4 L/kg) than those of Trimethoprim (TMP) in pig, calf, monkey, sheep and some other animal species, and a similar pattern is observed for Aditoprime where the distribution volume is about four times higher than that of TMP[1]. Aditoprime (10 -40 mg/kg; b.w.; intramuscularly) shows efficacy in infected swine (swine streptococcosis)[1].
References

[1]. Then RL, et al. Properties of aditoprim, a new antibacterial dihydrofolate reductase inhibitor. Zentralbl Veterinarmed B. 1988;35(2):114-120.

[2]. Cheng G, et al. The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis. Sci Rep. 2017;7:41370. Published 2017 Feb 1.

[3]. Wang X, et al. Two-generation reproduction and teratology studies of feeding aditoprim in Wistar rats. J Appl Toxicol. 2015;35(12):1531-1538.

Chemical & Physical Properties

Density1.233g/cm3
Boiling Point503.9ºC at 760 mmHg
Molecular FormulaC15H21N5O2
Molecular Weight303.36000
Flash Point258.5ºC
Exact Mass303.17000
PSA100.98000
LogP1.17520
Index of Refraction1.633
InChIKeyQBQMXWZTRRWPGK-UHFFFAOYSA-N
SMILESCOc1cc(Cc2cnc(N)nc2N)cc(OC)c1N(C)C

Safety Information

Hazard CodesXi

Synonyms

Aditoprima
Aditoprim
Aditoprime
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