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OPC-167832

(Synonyms: Quabodepistat, OPC167832, OPC 167832) Copy Product Info
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Synonyms: Quabodepistat, OPC167832, OPC 167832

Catalog No. T37880 Copy Product Info
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OPC-167832 is a highly potent and orally bioavailable dprE1 inhibitor with an IC₅₀ of 0.258 μM. It exhibits anti-mycobacterial activity against Mycobacterium tuberculosis and can be used in tuberculosis-related research.
OPC-167832
Cas No. 1883747-71-4
Pack SizePriceUSA StockGlobal StockQuantity
25 mg$1,17010-14 weeks10-14 weeks
50 mg$1,53010-14 weeks10-14 weeks
100 mg$2,44010-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
OPC-167832 is a highly potent and orally bioavailable dprE1 inhibitor with an IC₅₀ of 0.258 μM. It exhibits anti-mycobacterial activity against Mycobacterium tuberculosis and can be used in tuberculosis-related research.
In vitro
Methods: In vitro drug sensitivity testing of OPC-167832 was performed on Mycobacterium tuberculosis and various standard strains, and its bacteriostatic and bactericidal activities against intracellular Mycobacterium tuberculosis were determined.
Results:
1 OPC-167832 exhibited potent inhibitory activity against the Mycobacterium tuberculosis laboratory strains H37Rv and Kurono, with a MIC of 0.0005 μg/mL for both, while it had almost no antibacterial activity against standard strains of aerobic and anaerobic non-mycobacterial bacteria.
2 The IC₉₀ of OPC-167832 against intracellular Mycobacterium tuberculosis was less than 100%, and the bacteriostatic concentrations against H37Rv and Kurono strains were 0.0048 μg/mL and 0.0027 μg/mL, respectively; it could exert intracellular bactericidal effect at low concentrations, and the bactericidal activity tended to be saturated when the concentration was ≥0.004 μg/mL [1].
In vivo
Methods: OPC-167832 was administered orally at doses of 0.625–10 mg/kg to detect its pharmacokinetics and lung tissue distribution; oral administration at the same doses was performed for 4 weeks to observe changes in lung tissue CFU; intragastric administration of 2.5 mg/kg combined with DCMB was conducted for 12 weeks to evaluate the combined therapeutic effect.
Results:
1 OPC-167832 had good pharmacokinetic properties after oral administration, with a time to peak concentration (tmax) of 0.5–1.0 h and an elimination half-life (t1/2) of 1.3–2.1 h; the drug concentration in the lungs was approximately twice that in the plasma, and the Cmax and AUCt in both plasma and lungs were dose-dependent.
2 Compared with the vehicle group, OPC-167832 (0.625–10 mg/kg, oral administration, 4 weeks) significantly reduced lung CFU, and the lung CFU decreased in a dose-dependent manner within the dose range of 0.625–2.5 mg/kg.
3 OPC-167832 (2.5 mg/kg, intragastric administration, combined with DCMB, 12 weeks) showed the optimal therapeutic effect; the lung CFU of mice was below the detection limit after 6 weeks of treatment, and the lung bacteria of all mice were eradicated after 8 weeks of treatment [1].
SynonymsQuabodepistat, OPC167832, OPC 167832
Chemical Properties
Molecular Weight456.84
FormulaC21H20ClF3N2O4
Cas No.1883747-71-4
SmilesO(C[C@@]1(O)[C@H](O)CN(CC1)C2=C(F)C=C(Cl)C=C2F)C3=C4C(=C(F)C=C3)NC(=O)CC4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 144 mg/mL (315.21 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1890 mL10.9448 mL21.8895 mL109.4475 mL
5 mM0.4378 mL2.1890 mL4.3779 mL21.8895 mL
10 mM0.2189 mL1.0945 mL2.1890 mL10.9448 mL
20 mM0.1094 mL0.5472 mL1.0945 mL5.4724 mL
50 mM0.0438 mL0.2189 mL0.4378 mL2.1890 mL
100 mM0.0219 mL0.1094 mL0.2189 mL1.0945 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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2 Enter the in vivo formulation:
% DMSO
%
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% Saline/PBS/ddH2O

Dose Conversion

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Keywords

Related Tags: OPC-167832 chemical structure | OPC-167832 in vivo | OPC-167832 in vitro | OPC-167832 formula | OPC-167832 molecular weight