Art. -Nr.: HY-134940

Quabodepistat

(Synonyms: OPC-167832)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with an IC₅₀ of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis.

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Reinheit: 98.03%
CAS. Nr.: 1883747-71-4
Formel: C₂₁H₂₀ClF₃N₂O₄
Molecular Weight:456.84

Speicherung:

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

Quabodepistat Chemical Structure

CAS. Nr.: 1883747-71-4

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Quabodepistat (OPC-167832) exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, Quabodepistat has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria^[1].
The IC₉₀ values of Quabodepistat against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. Quabodepistat shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher^[1].

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

In Vivo

Quabodepistat (OPC-167832) (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (t_max) and is eliminated with a half-life (t_1/2) of 1.3 h to 2.1 h Quabodepistat distribution in the lungs is approximately 2 times higher than that in plasma, and the C_max and AUC_t of Quabodepistat in plasma and the lungs shows dose dependency^[1].
Quabodepistat (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. Quabodepistat combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone^[1].
^[1].
Quabodepistat (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate^[1].

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

Animal Model:

ICR mice^[1]
Dosage:

0.625-10 mg/kg
Administration:

Oral administration; 0.625-10 mg/kg; 4 weeks
Result:

Exhibited in vivo efficacy against a mouse chronic TB model.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1883747-71-4
Appearance Solid
Molecular Weight 456.84
Formel C₂₁H₂₀ClF₃N₂O₄
Color White to light yellow
SMILES

O=C1NC2=C(C(OC[C@@]3(O)[C@H](O)CN(C4=C(F)C=C(Cl)C=C4F)CC3)=CC=C2F)CC1
Synonyms

OPC-167832
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

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Journal Impact Factor

Antimicrob Agents Chemother

Multidrug tolerance conferred by loss-of-function mutations in anti-sigma factor RshA of Mycobacterium abscessus. [Abstract]

2024 Oct 29:e0105124. PMID: 39470195
bioRxiv

Structural and functional analysis of the Mycobacterium tuberculosis MmpS5L5 efflux pump presages a pathway to increased bedaquiline resistance. [Abstract]

2025 Jun 24:2025.06.24.661325. PMID: 40667120
bioRxiv

2025 February 06.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 180 mg/mL (394.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1890 mL

10.9448 mL

21.8895 mL

5 mM

0.4378 mL

2.1890 mL

4.3779 mL

10 mM

0.2189 mL

1.0945 mL

2.1890 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 4.5 mg/mL (9.85 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1890 mL	10.9448 mL	21.8895 mL	54.7238 mL
	5 mM	0.4378 mL	2.1890 mL	4.3779 mL	10.9448 mL
	10 mM	0.2189 mL	1.0945 mL	2.1890 mL	5.4724 mL
	15 mM	0.1459 mL	0.7297 mL	1.4593 mL	3.6483 mL
	20 mM	0.1094 mL	0.5472 mL	1.0945 mL	2.7362 mL
	25 mM	0.0876 mL	0.4378 mL	0.8756 mL	2.1890 mL
	30 mM	0.0730 mL	0.3648 mL	0.7297 mL	1.8241 mL
	40 mM	0.0547 mL	0.2736 mL	0.5472 mL	1.3681 mL
	50 mM	0.0438 mL	0.2189 mL	0.4378 mL	1.0945 mL
	60 mM	0.0365 mL	0.1824 mL	0.3648 mL	0.9121 mL
	80 mM	0.0274 mL	0.1368 mL	0.2736 mL	0.6840 mL
	100 mM	0.0219 mL	0.1094 mL	0.2189 mL	0.5472 mL

Keywords

Quabodepistat

3 Cited Publications

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Quabodepistat

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Anti-tuberculosis Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Quabodepistat

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Quabodepistat

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Antibacterial Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Anti-tuberculosis Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Quabodepistat

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Quabodepistat Related Classifications

HY-134940 Related Classifications