1. Anti-infection
  2. Bacterial
  3. MmpL3-IN-1

MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis.

For research use only. We do not sell to patients.

MmpL3-IN-1 Chemical Structure

MmpL3-IN-1 Chemical Structure

CAS No. : 2290534-93-7

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Description

MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis[1].

Cellular Effect
Cell Line Type Value Description References
Vero IC50
35.3 μg/mL
Compound: 32
Cytotoxicity against African green monkey vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against African green monkey vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 35915958]
In Vitro

MmpL3-IN-1 (compound 32) (0.26-64 μg/mL, 2-7days) has potent anti-M. tuberculosis activity with the MIC value of less than 0.016 μg/mL and with almost non-toxic to Vero cells[1].
MmpL3-IN-1 has good microsomal stability and little inhibition of hERG K+ channels with the IC50 value of more than 30 μM[1].
MmpL3-IN-1 (0.0625-1 μg/mL, 16 h) can inhibit TMM transport by targeting MmpL3, thereby affecting the formation of the cell wall of M. tuberculosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Vero cells
Concentration: 0.26-64 μg/mL
Incubation Time: 48 hours
Result: Inhibited cell viability with an IC50 value of 35.3 μg/mL.

Western Blot Analysis[1]

Cell Line: M. tuberculosis H37Rv mc2 6206
Concentration: 0.0625-1 μg/mL
Incubation Time: 16 hours
Result: Resulted in the accumulation of alginate monomycin (TMM) expression and reduced cell wall-bound mycolic acid methyl esters (MAMEs) in a dose-dependent manner.
Reduced synthesis of alginate dimycolate (TDM), together with accumulation of free mycolate at high concentration.
In Vivo

MmpL3-IN-1 (compound 32) (oral gavage, 100 mg/kg, 5 days per week, 30 days) has effective anti-tuberculosis activity in SPF BALB/c female mice with H37Rv[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SPF BALB/c female mice with H37Rv[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 5 days per week; 30 days
Result: Showed a 2.0 log CFU reduction of H37Rv in lung colony forming units.
Animal Model: BALB/c mouse (female) weighing 20-25 g[1]
Dosage:
Administration: 100 mg/kg p.o. or 10 mg/kg i.v. ; 0-24 hours
Result: b>The pharmacokinetic parameters of MmpL3-IN-1 (compound 32)
Parameter iv, 10 mg/kg po, 100 mg/kg
t1/2(h) 7.37 7.48
Cmax (ng/mL) 5105 211
Tmax(h) 0.03 0.5
AUC0-t(h•ng/mL) 2475 1625
MRT0-t(h•ng/mL) 2.00 8.69
V (mL/kg) 42067 -
CL (mL/h/kg) 3958 -
F% - 6.6
Molecular Weight

357.40

Formula

C20H21F2N3O

CAS No.
SMILES

O=C(C1=CC(C2=CC=C(F)N=C2F)=CN1)NC3C4CC5CC(C4)CC3C5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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MmpL3-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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