TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis [1].
In Vivo, TGFBR1-IN-2 (10 mg/kg. p.o.) demonstrates a short half-life and low plasma concentration in CD1 mice, with T1/2 of 1.8 h, Cmax of 280 ng/ mL and AUClast of 640 h*ng/mL[1].
In Vitro, TGFBR1-IN-2 inhibits nonreplicating Mycobacterium tuberculosis, with MIC90NR of 1 μM, MIC90 of 20 μM, MIC50 of 16 μM[1]. TGFBR1-IN-2 (2-20 μM, 35 days) inhibits drug-tolerant microorganisms (Mycobacterium tuberculosis-GFP culture with Rifampicin and Isoniazid )[1].
References:
[1]. Nandakumar, et al. Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline. Journal of medicinal chemistry. 2023, 66(21):14724-14734.
In Vivo, TGFBR1-IN-2 (10 mg/kg. p.o.) demonstrates a short half-life and low plasma concentration in CD1 mice, with T1/2 of 1.8 h, Cmax of 280 ng/ mL and AUClast of 640 h*ng/mL[1].
In Vitro, TGFBR1-IN-2 inhibits nonreplicating Mycobacterium tuberculosis, with MIC90NR of 1 μM, MIC90 of 20 μM, MIC50 of 16 μM[1]. TGFBR1-IN-2 (2-20 μM, 35 days) inhibits drug-tolerant microorganisms (Mycobacterium tuberculosis-GFP culture with Rifampicin and Isoniazid )[1].
References:
[1]. Nandakumar, et al. Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline. Journal of medicinal chemistry. 2023, 66(21):14724-14734.