1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. AZD8797

AZD8797 

Cat. No.: HY-13848 Purity: 98.22%
Handling Instructions

AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.

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

AZD8797 Chemical Structure

AZD8797 Chemical Structure

CAS No. : 911715-90-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
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100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE AZD8797

    AZD8797 purchased from MCE. Usage Cited in: J Cancer. 2018 Sep 8;9(19):3603-3612.

    MDA-MB-231 cells are pretreated with the CX3CR1 antagonist AZD8797, and stimulated by CX3CL1 for 30 mins, the phosphorylation levels of Src and FAK are detected. CX3CL1-only group as control.

    View All CXCR Isoform Specific Products:

    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.

    IC50 & Target[3]

    [125I]-CX3CL1-CX3CR1

    3.9 nM (Ki, in HEK293S cells)

    125I-IL-8-CXCR2

    2800 nM (Ki, in HEK293S cells)

    In Vitro

    In a flow adhesion assay, AZD8797 antagonizes the natural ligand, fractalkine (CX3CL1), in both human whole blood (hWB) and in a B-lymphocyte cell line with IC50 values of 300 and 6 nM respectively. AZD8797 also prevents G-protein activation in a [35S]GTPγS accumulation assay. AZD8797 positively modulates the CX3CL1 response at sub-micromolar concentrations in a β-arrestin recruitment assay. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd[1]. AZD8797 binds selectively with high affinity to human and rat CX3CR1 (Ki of hCX3CR1, 4 nM; Ki of rCX3CR1, 7 nM, respectively). The equilibrium dissociation constant, KB, demonstrates that AZD8797 is a very potent inhibitor for human CX3CR1 (10 nM). The potency is threefold lower for rat CX3CR1 (29 nM) and decreases even further at mouse CX3CR1 (54 nM)[2].

    In Vivo

    AZD8797 treatment in Dark Agouti rats with myelin oligodendrocyte glycoprotein-induced EAE results in reduced paralysis, CNS pathology, and incidence of relapses. The compound is effective when starting treatment before onset, as well as after the acute phase[2].

    Molecular Weight

    403.56

    Formula

    C₁₉H₂₅N₅OS₂

    CAS No.

    911715-90-7

    SMILES

    CC(C)C[[email protected]@H](NC1=NC(S[[email protected]@H](C)C2=CC=CC=C2)=NC3=C1SC(N)=N3)CO

    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 : ≥ 150 mg/mL (371.69 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4779 mL 12.3897 mL 24.7795 mL
    5 mM 0.4956 mL 2.4779 mL 4.9559 mL
    10 mM 0.2478 mL 1.2390 mL 2.4779 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    CHO-hCX3CR1 membranes together with different concentrations of AZD8797 are incubated in 50 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 10 μM GDP and 0.01% gelatin in a MicroWell 96-well plate. 0.56 μCi/mL [35S]GTPγS and EC80 of CX3CL1 are then added. The plate is incubated at 30°C for 1 h and subsequently unbound [35S]GTPγS is separated from bound by vacuum filtration to a Printed Filtermat B. The different AZD8797 concentrations are achieved by stepwise dilution in DMSO to achieve a final DMSO concentration of 1% in all wells after addition of assay buffer, regardless of AZD8797 concentration[1].

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

    Animal Administration
    [2]

    Rats: AZD8797 is formulated in 30–35% (wt/wt) hydroxy-propyl-beta-cyklodextrin and administered s.c. through osmotic minipumps. Treatment is blinded to the operator. The plasma concentration of AZD8797 is analyzed twice from each rat[2].

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

    References
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