Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MmpL3-IN-1, also known as compound 32, is a highly effective inhibitor of Mycobacterial membrane protein large 3 (MmpL3). With an anti-tuberculosis activity exhibiting a minimum inhibitory concentration (MIC) of less than 0.016 μg/mL in M. tuberculosis, MmpL3-IN-1 is a valuable compound for research on drug-resistant tuberculosis [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | MmpL3-IN-1, also known as compound 32, is a highly effective inhibitor of Mycobacterial membrane protein large 3 (MmpL3). With an anti-tuberculosis activity exhibiting a minimum inhibitory concentration (MIC) of less than 0.016 μg/mL in M. tuberculosis, MmpL3-IN-1 is a valuable compound for research on drug-resistant tuberculosis [1]. |
In vitro | MmpL3-IN-1 (compound 32) demonstrated potent anti-M. tuberculosis activity, with a minimal inhibitory concentration (MIC) below 0.016 μg/mL over a treatment duration of 2-7 days at varying dosages of 0.26-64 μg/mL, and showed minimal toxicity towards Vero cells. This compound exhibited good microsomal stability and negligible inhibition of hERG K+ channels, with an IC50 value exceeding 30 μM. Furthermore, at concentrations ranging from 0.0625-1 μg/mL over 16 hours, MmpL3-IN-1 specifically inhibited the transport of trehalose monomycolate (TMM), disrupting the cell wall formation of M. tuberculosis by targeting MmpL3. Assays revealed that, in Vero cells treated for 48 hours with 0.26-64 μg/mL, cell viability was inhibited, showing an IC50 value of 35.3 μg/mL. Similarly, a western blot analysis on M. tuberculosis H37Rv mc^26206 exposed to 0.0625-1 μg/mL for 16 hours highlighted a dose-dependent increase in TMM and a decrease in cell wall-bound mycolic acid methyl esters (MAMEs), indicating that high concentrations of MmpL3-IN-1 reduce the synthesis of trehalose dimycolate (TDM) and accumulate free mycolate. |
In vivo | MmpL3-IN-1 (compound 32), when administered orally at a dosage of 100 mg/kg for 5 days a week over a period of 30 days, demonstrated potent anti-tuberculosis efficacy in SPF BALB/c female mice infected with H37Rv, achieving a significant 2.0 log reduction in lung colony-forming units of H37Rv. In addition, when administered either orally (p.o.) at 100 mg/kg or intravenously (i.v.) at 10 mg/kg, MmpL3-IN-1 exhibited notable pharmacokinetic properties, including half-life (t 1/2), maximum concentration (Cmax), time to reach maximum concentration (Tmax), area under the plasma drug concentration-time curve from 0 to the last measurable concentration (AUC 0-t), mean residence time (MRT 0-t), volume of distribution (V), clearance (CL), and oral bioavailability (F%). Specifically, oral administration showed a half-life of about 7.48 hours with peak concentrations reached within 0.5 hours, while intravenous administration demonstrated a quicker Tmax at 0.03 hours, reflecting its rapid absorption and distribution within the body. |
Molecular Weight | 357.4 |
Formula | C20H21F2N3O |
CAS No. | 2290534-93-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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MmpL3-IN-1 2290534-93-7 inhibitor inhibit