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].

细胞效力
(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]
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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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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