1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Brensocatib

Brensocatib  (Synonyms: AZD7986; INS 1007)

Cat. No.: HY-101056 Purity: 99.88%
COA Handling Instructions

Brensocatib (AZD7986) is an oral dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.

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

Brensocatib Chemical Structure

Brensocatib Chemical Structure

CAS No. : 1802148-05-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
50 mg USD 900 In-stock
100 mg USD 1450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Brensocatib (AZD7986) is an oral dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively[1].

IC50 & Target

DPP-1

 

In Vitro

Results from cell assay show that Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. Brensocatib is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of Brensocatib (38 pM to 10 μM), concentration-dependent decreases in cell lysate enzyme activity are observed for DPP1, as well as for all of the three NSPs, NE, Pr3, and CatG. Brensocatib inhibits activation of all three NSPs in a concentration dependent manner, with pIC50 values of around 7 for all three NSPs. The reduction of the activities is almost complete, with NE, Pr3, and CatG activities reduced to 4 to 10% of control at 10 μM Brensocatib[1].

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

In Vivo

Brensocatib (AZD7986) shows good stability in plasma, with a half life of >10 h. Brensocatib inhibits activation of NE and Pr3, but not CatG, in bone marrow cell lysates in a dose dependent manner in vivo[1].

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

Clinical Trial
Molecular Weight

420.46

Formula

C23H24N4O4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@H]1OCCCNC1)N[C@H](C#N)CC2=CC=C(C3=CC=C(OC(N4C)=O)C4=C3)C=C2

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 : 100 mg/mL (237.83 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 2.3783 mL 11.8917 mL 23.7835 mL
5 mM 0.4757 mL 2.3783 mL 4.7567 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Purity: 99.88%

References
Cell Assay
[1]

Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5×105 cells/mL per well. Added to this is 10 μL of Brensocatib at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values[1].

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

Animal Administration
[1]

Rats are used for the in vivo study. Naive rats are dosed orally twice daily with Brensocatib at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases (NSPs) activity analysis using commercial synthetic peptide substrates[1].

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, 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 2.3783 mL 11.8917 mL 23.7835 mL 59.4587 mL
5 mM 0.4757 mL 2.3783 mL 4.7567 mL 11.8917 mL
10 mM 0.2378 mL 1.1892 mL 2.3783 mL 5.9459 mL
15 mM 0.1586 mL 0.7928 mL 1.5856 mL 3.9639 mL
20 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9729 mL
25 mM 0.0951 mL 0.4757 mL 0.9513 mL 2.3783 mL
30 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9820 mL
40 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
50 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
60 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9910 mL
80 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 mL
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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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Brensocatib
Cat. No.:
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