2. Anti-infection
  3. Bacterial
  4. Quabodepistat

Quabodepistat  (Synonyms: OPC-167832)

Cat. No.: HY-134940 Purity: 98.00%
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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.

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

Quabodepistat Chemical Structure

Quabodepistat Chemical Structure

CAS No. : 1883747-71-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 560 In-stock
25 mg USD 1150 In-stock
50 mg USD 1850 In-stock
100 mg USD 2950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Quabodepistat Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

Quabodepistat Related Antibodies
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 (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h Quabodepistat distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt 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
Molecular Weight

456.84

Formula

C21H20ClF3N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1890 mL 10.9448 mL 21.8895 mL
5 mM 0.4378 mL 2.1890 mL 4.3779 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, 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.

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 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
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Quabodepistat 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.

Keywords:

Quabodepistat1883747-71-4OPC-167832OPC167832OPC 167832BacterialtuberculosisTBDprE1antituberculosisinfectious diseaseInhibitorinhibitorinhibit

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