Brensocatib (Synonyms: AZD7986; INS 1007)

Name: Brensocatib
Brand: MedChemExpress
SKU: HY-101056
Rating: 5.0 (7 reviews)

Cat. No.: HY-101056 Purity: 99.88%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 1802148-05-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	Get quote
10 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Brensocatib:

Brensocatib (Standard) Get quote

7 Publications Citing Use of MCE Brensocatib

•bioRxiv. 2023 Nov 5.

In Vivo Efficacy Study

Histological Imaging/Staining

ELISA

Cell Imaging/Staining

: Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]; Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily) effectively restored body weight and extended overall survival of mice after orthotopic injection of 4T1 cells.

: Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]; Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily). NET staining and quantitation in lungs of mice after orthotopic injection of 4T1.

: Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]; Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily). Lung-metastatic nodules at week 7 of mice after orthotopic injection of AT3.

: Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]; Brensocatib (AZD7986) (5 mg/kg; p.o.; twice daily) suppressed circulating IL-1b levels in the mice after orthotopic injection of AT3.

: Brensocatib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]; NETosis of murine neutrophils was pre-treated with Brensocatib (AZD7986) (10 μM).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

View All Isoforms

DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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

Cellular Effect

Cell Line	Type	Value	Description	References
L02	IC₅₀	> 100 μM Compound: AZD7986	Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 34374541]

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.

1802148-05-5

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
10 mM	0.2378 mL	1.1892 mL	2.3783 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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%

Select Batch:

Data Sheet (274 KB) SDS (643 KB)

COA (247 KB) HNMR (267 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472. [Content Brief]

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	[1]. Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472. [Content Brief]

Complete Stock Solution Preparation Table

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

Brensocatib Related Classifications

Inflammation/Immunology

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:

Brensocatib1802148-05-5AZD7986 INS 1007AZD 7986AZD-7986INS1007INS 1007INS-1007Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Brensocatib (Synonyms: AZD7986; INS 1007)

Customer Review

Other Forms of Brensocatib:

Brensocatib Related Antibodies

7 Publications Citing Use of MCE Brensocatib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Brensocatib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Brensocatib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report