1. Anti-infection
  2. Bacterial

BTZ043 

Cat. No.: HY-13579
Handling Instructions

BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.

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

BTZ043 Chemical Structure

BTZ043 Chemical Structure

CAS No. : 1161233-85-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
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100 mg USD 850 In-stock
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Other Forms of BTZ043:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.

IC50 & Target

DprE1[1].

In Vitro

The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis are 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively[2]. The in vitro activity of BTZ043 against 30 Nocardia brasiliensis isolates is also tested. The MIC50 and MIC90 values for BTZ043 are 0.125 and 0.25 μg/mL. The MIC for N. carnea ATCC 6847 is 0.003μg/mL, for N. transvalensis ATCC 6865 is 0.003μg/mL, for N. brasiliensis NCTC10300 is 0.03 μg/mL, and for N. brasiliensis HUJEG-1 is 0.125μg/mL. The MIC value for M. tuberculosis H37Rv is 0.000976 μg/mL. The MIC value of BTZ-043 is >64 μg/mL for Escherichia coli ATCC 25922 and S. aureus ATCC 29213[3].

In Vivo

Four weeks of treatment with BTZ043 reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional results suggest that BTZ043 efficacy is time-rather than dose-dependent. Acute (5 g/kg) and chronic (25 and 250 mg/kg) toxicology studies in uninfected mice show that, even at the highest dose tested, there are no adverse anatomical, behavioral, or physiological effects after one month[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 13.3 mg/mL (30.83 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3181 mL 11.5904 mL 23.1809 mL
5 mM 0.4636 mL 2.3181 mL 4.6362 mL
10 mM 0.2318 mL 1.1590 mL 2.3181 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice[2]
Animal efficacy is determined in a standard mouse infection model. BALB/c mice are infected with a low bacillary load (~200 CFU) of M. tuberculosis H37Rv via aerosol. Treatment started four-weeks post infection. Mice are dosed by gavage with 37.5, or 300 mg of BTZ043, per kg body weight, in carboxymethyl cellulose formulation (0.25%), once daily, six times/week, for four weeks. Control and treated mice are sacrificed, lungs and spleens homogenized and dilutions plated for enumeration of viable bacilli[2].

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

References
Molecular Weight

431.39

Formula

C₁₇H₁₆F₃N₃O₅S

CAS No.

1161233-85-7

SMILES

O=C1N=C(N(CC2)CCC32OC[[email protected]](C)O3)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BTZ043
Cat. No.:
HY-13579
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BTZ043

Cat. No.: HY-13579