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.
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- CAS. Nr.: 2290534-93-7
- Formel: C20H21F2N3O
- Molecular Weight:357.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
35.3 μg/mL
Compound: 32
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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
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[PMID: 35915958] |
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.
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Cell Line:Vero cells
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Concentration:0.26-64 μg/mL
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Incubation Time:48 hours
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Result:Inhibited cell viability with an IC50 value of 35.3 μg/mL.
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Cell Line:M. tuberculosis H37Rv mc2 6206
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Concentration:0.0625-1 μg/mL
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Incubation Time:16 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SPF BALB/c female mice with H37Rv[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; 5 days per week; 30 days
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Result:Showed a 2.0 log CFU reduction of H37Rv in lung colony forming units.
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Animal Model:BALB/c mouse (female) weighing 20-25 g[1]
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Dosage:
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Administration:100 mg/kg p.o. or 10 mg/kg i.v. ; 0-24 hours
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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
Chemical Information
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CAS. Nr. 2290534-93-7
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Molecular Weight 357.40
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Formel C20H21F2N3O
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SMILES
O=C(C1=CC(C2=CC=C(F)N=C2F)=CN1)NC3C4CC5CC(C4)CC3C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MmpL3-IN-1 Related Classifications
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