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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | 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. |
| Targets&IC50 | TGFβRI:0.01 μM (Kd) |
| In vitro | 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. |
| In vivo | 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. |
| Molecular Weight | 313.36 |
| Formula | C19H15N5 |
| Cas No. | 733806-89-8 |
| Smiles | N=1C=CC(=CC1)NC=2N=C(N=C3C=CC=CC32)C=4N=C(C=CC4)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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