2. Anti-infection
  3. Bacterial
  4. DprE1-IN-1

DprE1-IN-1 是一种有效且有口服活性的 DprE1 抑制剂，具有良好的肝细胞稳定性、低细胞毒性和低hERG通道抑制。DprE1-IN-1 对 DprE1-IN-1 对药敏和临床分离的耐药结核菌株均有有效抗性 (MICs<0.1 μg/mL)，以及在巨噬细胞内抗分支杆菌活性良好，能减少 1.29 log10CFU。

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DprE1-IN-1 Chemical Structure

DprE1-IN-1 Chemical Structure

CAS No. : 920459-41-2

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DprE1-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

IC50 & Target

MICs: <0.1 μg/mL (Tuberculosis strains)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 IC50
62.89 μg/mL
Compound: 17b
Cytotoxicity against human HepG2 cells measured by MTT assay
Cytotoxicity against human HepG2 cells measured by MTT assay
[PMID: 35101648]
J774.A1 IC50
> 64 μg/mL
Compound: 17b
Cytotoxicity against mouse J774.A1 cells measured by MTT assay
Cytotoxicity against mouse J774.A1 cells measured by MTT assay
[PMID: 35101648]
Vero IC50
58.18 μg/mL
Compound: 17b
Cytotoxicity against African green monkey Vero cells measured by MTT assay
Cytotoxicity against African green monkey Vero cells measured by MTT assay
[PMID: 35101648]
体外研究
(In Vitro)

DprE1-IN-1 (compound 17b) (64 to 0.26 μg/mL; 48 hours) has high safety with low cytotoxicity towards HepG2, J774A.1 macrophage cells (IC50>60 μg/mL) and Vero (IC50=58.18 μg/mL) alongside potent efficacy and good druggability[1].
DprE1-IN-1 can reduce 1.19 and 1.29 log10 CFU M. tuberculosis in J774A.1 macrophages at 5 μg/mL and 10 μg/mL, respectively, for 3 days treatment[1].
DprE1-IN-1 (compound 17b) (1 μM; 0-120 minutes) has high stability in human and mice hepatocytes (remaining of 42% and 49.7%, respectively; t1/2 of 24.0 and 29.7 min, respectively)[1].

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

DprE1-IN-1 相关抗体:

Cell Cytotoxicity Assay

Cell Line: Vero, HepG2 and mouse J774A.1 macrophage cells[1]
Concentration: 64 to 0.26 μg/mL
Incubation Time: 48 hours
Result: Displayed high safety with low cytotoxicity towards HepG2, J774A.1 macrophage cells (IC50>60 μg/mL) and Vero (IC50=58.18 μg/mL) alongside potent efficacy and good druggability.
体内研究
(In Vivo)

DprE1-IN-1 (100 mg/kg; oral gavage; 5 days per week from day 10 until day 30) can reduce the bacterial burden in the lungs by 0.54 log10 CFU after three weeks of treatment in M. tuberculosis H37Rv infected mice[1].

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

Animal Model: Female SPF Balb/c mice (18-20 g) (M. tuberculosis H37Rv infected)[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 5 days per week from day 10 until day 30
Result: Reduced the bacterial burden in the lungs by 0.54 log10 CFU compared with the untreated control group after three weeks of treatment.
分子量

451.52

Formula

C19H21N3O6S2
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

DprE1-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

DprE1-IN-1920459-41-2BacterialThiophene-benzenesulfonamideDrug-resistant tuberculosisOralHepatocyte stabilityLow cytotoxicityAntimycobacterial activityInhibitorinhibitorinhibit

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