1. Anti-infection
  2. Bacterial Antibiotic
  3. Macozinone

Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect.

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

Macozinone Chemical Structure

Macozinone Chemical Structure

CAS No. : 1377239-83-2

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect[1][2].

IC50 & Target

DprE1[1]

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
101.7 μM
Compound: PBTZ169
Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
[PMID: 31408806]
HepG2 IC50
18.98 μg/mL
Compound: 2; PBTZ169
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30336450]
Vero CC50
> 125 μM
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
[PMID: 25754492]
Vero IC50
> 64 μg/mL
Compound: 2; PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30336450]
Vero CC50
> 64 μg/mL
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
[PMID: 33823392]
Vero CC50
1402.82 μM
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 28626525]
Vero CC50
31 μg/mL
Compound: PBTZ169
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30692025]
In Vitro

Macozinone (PBTZ169) is highly potent against M. tuberculosis in vitro, ex vivo, and in vivo[2].

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

Clinical Trial
Molecular Weight

456.48

Formula

C20H23F3N4O3S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC(C(F)(F)F)=CC([N+]([O-])=O)=C2SC(N3CCN(CC4CCCCC4)CC3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (14.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1907 mL 10.9534 mL 21.9068 mL
5 mM 0.4381 mL 2.1907 mL 4.3814 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.46%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1907 mL 10.9534 mL 21.9068 mL 54.7669 mL
5 mM 0.4381 mL 2.1907 mL 4.3814 mL 10.9534 mL
10 mM 0.2191 mL 1.0953 mL 2.1907 mL 5.4767 mL
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Macozinone Related Classifications

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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Product Name:
Macozinone
Cat. No.:
HY-12903
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