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

DprE1-IN-1 

Cat. No.: HY-144341
Handling Instructions

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 drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages.

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

DprE1-IN-1 Chemical Structure

DprE1-IN-1 Chemical Structure

CAS No. : 920459-41-2

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages[1].

IC50 & Target

MICs: <0.1 μg/mL (Tuberculosis strains)[1]

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.

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.
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.
Molecular Weight

451.52

Formula

C19H21N3O6S2

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DprE1-IN-1
Cat. No.:
HY-144341
Quantity:
MCE Japan Authorized Agent: