1. Immunology/Inflammation GPCR/G Protein
  2. CX3CR1 CXCR
  3. AZD8797

AZD8797  (Synonyms: KAND567)

Cat. No.: HY-13848 Purity: 98.73%
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AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 275 In-stock
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10 mM * 1 mL in DMSO USD 275 In-stock
Solid
5 mg USD 250 In-stock
10 mg USD 450 In-stock
25 mg USD 950 In-stock
50 mg USD 1500 In-stock
100 mg USD 2100 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

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    Description

    AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively[1].

    IC50 & Target[3]

    CX3CR1

    3.9 nM (Ki, 125I-CX3CL-CX3CR1 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].

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

    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].

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

    Molecular Weight

    403.56

    Formula

    C19H25N5OS2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C)C[C@@H](NC1=NC(S[C@@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 2 years
    -20°C 1 year
    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 5 mg/mL (12.39 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    • 4.

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

      Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation
    References
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    AZD8797 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.

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    Product Name:
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