Cas No.: | 1494675-86-3 |
Chemical Name: | AZ7371 |
Synonyms: | AZ7371;ZA7371;AZ-7371;DprE1-IN-1;TBA-7371 |
SMILES: | O=C(C1=CN(CC2=NC=NC(OC)=C2C)C3=CC(C)=CN=C31)NCCO |
Formula: | C18H21N5O3 |
M.Wt: | 355.391043424606 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | DprE1-IN-1 is a potent DprE1 inhibitor, with ic50 of 10 nM, also inhibits PDE6, with IC50 of 6 uM. |
In Vivo: | The pharmacokinetic profile of DprE1-IN-1 as a representative of the series in mice, rats, and dogs was determined after i.v. and oral dosing. DprE1-IN-1 shows oral bioavailabilities of 86% and 100% in rats and dogs, respectively. The oral exposures of DprE1-IN-1, assessed in infected animals, shows AUCs ranging from 166 to 240 μM · h, and free plasma concentrations were maintained above the MIC for 10 to 24 h. [2] |
References: | [1]. Shirude PS, et al. Lead optimization of 1,4-azaindoles as antimycobacterial agents. J Med Chem. 2014 Jul 10;57(13):5728-37. [2]. Chatterji M, et al. 1,4-azaindole, a potential drug candidate for treatment of tuberculosis. Antimicrob Agents Chemother. 2014 Sep;58(9):5325-31. |