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AZ-7371(TBA-7371)

  Cat. No.:  DC8842   Featured
Chemical Structure
1494675-86-3
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More than 5000 active chemicals with high quality for research!
Field of application
TBA-7371 (TBA7371, AZ 7371) is a potent, non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) with IC50 of 10 nM, an enzyme involved in mycobacterial cell wall biogenesis.TBA-7371 also inhibits PDE6 with an IC50 value of 4 uM.TBA-7371 is active against M. tuberculosis with an MIC range of 0.78-3.12 µM and demonstrates efficacy in a rodent model of tuberculosis.
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.
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