Aditoprime (Aditoprim) 是一种选择性细菌二氢叶酸还原酶(DHFR)抑制剂,可抑制二氢叶酸向四氢叶酸的转化。Aditoprime 抑制大肠杆菌和干酪乳杆菌 DHFR 的 IC50分别为 47 和 520 nM。Aditoprime 具有广谱抗菌、良好的抗菌活性和良好的药代动力学。
产品描述
Aditoprime (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 IC 50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics [1] [2] [3].
体外活性
Aditoprime 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 MIC 50 ≤ 4 μg/mL) [1].
体内活性
Aditoprime (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].
Cas No.
56066-63-8
分子式
C15H21N5O2
分子量
303.36
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years