2. Metabolic Enzyme/Protease Anti-infection Cell Cycle/DNA Damage
  3. Dihydroorotate Dehydrogenase SARS-CoV Virus Protease DNA/RNA Synthesis
  4. Brequinar

Brequinar  (Synonyms: DUP785; NSC 368390)

Cat. No.: HY-108325 Purity: 99.75%
COA Handling Instructions

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Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

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

Brequinar Chemical Structure

Brequinar Chemical Structure

CAS No. : 96187-53-0

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
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5 mg USD 84 In-stock
10 mg USD 132 In-stock
50 mg USD 330 In-stock
100 mg USD 520 In-stock
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Based on 12 publication(s) in Google Scholar

Other Forms of Brequinar:

Brequinar Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

In Vitro

Brequinar reduces virus progeny production by >90%, with EC50 of 17 nM. Brequinar (5 μM) also inhibits other orthopoxviruses, and blocks virus DNA replication. Brequinar does not affect virus early gene expression, but has a severe effect on the late stage of the virus cycle[1]. Brequinar reduces the level of envelope protein production and the viral titer in a dose-dependent manner, with EC50 of 78 nM in the CFI assay. Brequinar (5 μM) inhibits viral RNA synthesis. Brequinar has antiviral effect, but the effect is reversed by pyrimidine. Brequinar-resistant viruses can be selected in cell culture. Brequinar (5 μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons[2]. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC50 of 0.26 μM. Brequinar sodium effectively inhibits cell proliferation with an IC50 of 0.26 μM. Brequinar sodium inhibits autophosphorylation of p56lck with IC50 of 70 μM; inhibition is 39, 41, and 60% for 25, 50, and 100 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p56lck of the exogenous substrate, histone 2B, with an IC50 of 70 μM; inhibition is 10, 43, 59, and 86% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium inhibits autophosphorylation of p59fyn with an IC50 of 105 μM; inhibition is 0, 17, 48, and 65% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59fyn of histone 2B with an IC50 of 20 μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200 μM Brequinar sodium, respectively[3].

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

Brequinar Related Antibodies
In Vivo

Brequinar sodium-treated (10-20 mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with untreated BALB/c mice. Brequinar sodium reduces UTP and CTP levels in bone marrow cells by 30 and 25%, respectively. Brequinar sodium (10-20 mg/kg/day) in combination with uridine (1000-2000 mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls[3].

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

375.37

Formula

C23H15F2NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)C(C2=CC=C(C3=CC=CC=C3F)C=C2)=NC4=CC=C(F)C=C14)O
Shipping

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

DMSO : 25 mg/mL (66.60 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 2.6640 mL 13.3202 mL 26.6404 mL
5 mM 0.5328 mL 2.6640 mL 5.3281 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

Mass
=
Concentration
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.08 mg/mL (5.54 mM); Suspended solution; Need ultrasonic and warming

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Purity: 99.75%

COA (250 KB) HNMR (283 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[3]

Immunoprecipitated p59fyn or p56lck from CTLL-4 cells or LSTRA cells (5×106) is preincubated with various concentrations of BQR in the PTK buffer (50 mM HEPES (pH 7.4), 10 mM MgCl2, and 10 mM MnCl2) on ice for 10 min. Exogenous substrate, histone 2B (2 μg), is added and, after 10 min, the reaction is initiated by addition of 10 μCi [γ-32P]ATP. After incubation at 20°C for 10 min, the reaction mixture is subjected to electrophoresis in a 12.5% SDS-polyacrylamide gel. Phosphorylation of the kinase and the exogenous substrate is analyzed by autoradiography.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

The neutral-red uptake assay is used to evaluate cell viability. BSC-40 cells are seeded in 96-well plates in the presence of concentrations of Brequinar ranging from 0.01 μM to 75 μM for 24 h. Control cells are incubated with 0.1% DMSO. Neutral red is methanol/acetic acid-extracted from cells and is quantitated at an absorbance of 490 nm (A490). All measurements expressed the average of four independent assays.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Brequinar is administered once daily by i.p. injection, while uridine is administered twice daily. Mice are bled through the orbital vein using a microhematocrit capillary tube, and the blood is centrifuged for 10 min at 550 × g. The percentage of packed cell volumes is determined with a microhematocrit capillary tube reader. All mice are killed 4 h after receiving their last dose of Brequinar or uridine.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6640 mL 13.3202 mL 26.6404 mL 66.6010 mL
5 mM 0.5328 mL 2.6640 mL 5.3281 mL 13.3202 mL
10 mM 0.2664 mL 1.3320 mL 2.6640 mL 6.6601 mL
15 mM 0.1776 mL 0.8880 mL 1.7760 mL 4.4401 mL
20 mM 0.1332 mL 0.6660 mL 1.3320 mL 3.3300 mL
25 mM 0.1066 mL 0.5328 mL 1.0656 mL 2.6640 mL
30 mM 0.0888 mL 0.4440 mL 0.8880 mL 2.2200 mL
40 mM 0.0666 mL 0.3330 mL 0.6660 mL 1.6650 mL
50 mM 0.0533 mL 0.2664 mL 0.5328 mL 1.3320 mL
60 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1100 mL
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Brequinar 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:

Brequinar96187-53-0DUP785 NSC 368390DUP 785DUP-785NSC368390NSC 368390NSC-368390Dihydroorotate DehydrogenaseSARS-CoVVirus ProteaseDNA/RNA SynthesisDHODHSARS coronavirusInhibitorinhibitorinhibit

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