TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor (KD: 0.01 μM) and antimicrobial agent. It serves as a substrate for cytochrome P450. The compound contains a pyridyl-6-methyl group, essential for inhibiting Mycobacterium tuberculosis, and effectively inhibits non-replicating and persistent strains of this bacterium.

TGFβRI:0.01 μM (Kd)

TGFBR1-IN-2 exhibits bacteriostatic activity against non-replicating Mycobacterium tuberculosis, with a MIC 90NR of 1 μM, MIC 90 of 20 μM, and MIC 50 of 16 μM. Over 35 days, TGFBR1-IN-2 (2-20 μM) demonstrates inhibitory effects against drug-tolerant microorganisms, including cultures of Mycobacterium tuberculosis-GFP containing rifampicin and isoniazid.

TGFBR1-IN-2 (10 mg/kg, p.o.) has a short half-life and low plasma concentration in CD1 mice, with a T 1/2 of 1.8 hours, a C max of 280 ng/mL, and an AUC last of 640 h*ng/mL.