1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. AZD7986

AZD7986 (Synonyms: INS 1007)

Cat. No.: HY-101056 Purity: 99.07%
Handling Instructions

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.

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

AZD7986 Chemical Structure

AZD7986 Chemical Structure

CAS No. : 1802148-05-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 416 In-stock
Estimated Time of Arrival: December 31
1 mg USD 150 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

pIC50: 6.85 (human DPP1), 7.6 (mouse DPP1), 7.7 (rat DPP1), 7.8 (dog DPP1), 7.8 (rabbit DPP1)[1]

In Vitro

Results from cell assay show that 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. AZD7986 is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of AZD7986 (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. AZD7986 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 AZD7986[1].

In Vivo

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

Clinical Trial
Molecular Weight

420.46

Formula

C₂₃H₂₄N₄O₄

CAS No.

1802148-05-5

SMILES

O=C([[email protected]]1OCCCNC1)N[[email protected]](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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (237.83 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Activation of neutrophil serine proteases (NSPs) is assessed in vitro using primary bone marrow derived CD34+ neutrophil progenitor cells. Cells are cultured in media supplemented with rhSCF and rhIL-3 for 7 days, and then for a further 7 days in the presence of G-CSF and different concentrations of AZD7986 (38 pM to 10 μM). After harvesting and lysis with 10% Triton X-100 buffer, cell lysates are kept at -20°C until NSP activity analysis[1].

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

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 AZD7986 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 AZD7986 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
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AZD7986
Cat. No.:
HY-101056
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