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

MmpL3-IN-1 (compound 32) 是一种有效的霉菌膜大型蛋白 3 (MmpL3) 抑制剂。MmpL3-IN-1 具有抗结核活性,作用于 M. tuberculosis 的 MIC < 0.016 μg/mL,可用于耐药结核病的研究。

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MmpL3-IN-1 Chemical Structure

MmpL3-IN-1 Chemical Structure

CAS No. : 2290534-93-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(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].

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.
体内研究
(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].

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
分子量

357.40

Formula

C20H21F2N3O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献

MmpL3-IN-1 相关分类

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  • 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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