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AZD8797

SKU: orb1707606

Description

AZD8797 (KAND567) is a selective, orally bioavailable antagonist of human CX3CR1 and CXCR2. It has shown potential in research models to protect against SARS-CoV-2-related neuronal damage and to attenuate migraine-associated nociceptive sensitization and microglial activation in post-seizure rats.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number911715-90-7
MW403.56
Purity99.68%
FormulaC19H25N5OS2
SMILESCC(C)C[C@H](CO)Nc1nc(S[C@@H](C)c2ccccc2)nc2nc(N)sc12
TargetCXCR
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.91 mM);DMSO:100 mg/mL (247.79 mM)

Bioactivity

Target IC50
B-lymphocyte cells:6 nM|WB (human):300 nM|CX3CR1 (rat):7 nM (Ki)|CX3CR1:10 nM (human)|CX3CR1:29 nM (Rat)|CX3CR1:54 nM (mouse)|CX3CR1 (human):4 nM (Ki)|[125I]-CX3CL1-CX3CR1:3.9 nM (Ki, HEK293S cells)|[125I]-IL8-CXCR2:2800 nM (Ki, HEK293S cells)
In Vivo
Treatment with AZD8797 in Dark Agouti rats with myelin oligodendrocyte glycoprotein-induced EAE results in reduced paralysis, CNS pathology, and incidence of relapses. The compound is effective both when starting treatment before onset and after the acute phase.
In Vitro
In a flow adhesion assay, AZD8797, with IC50 values of 300 nM in human whole blood (hWB) and 6 nM in a B-lymphocyte cell line, antagonizes the natural ligand fractalkine (CX3CL1). AZD8797 also prevents G-protein activation in a [35S]GTPγS accumulation assay and positively modulates the CX3CL1 response in a β-arrestin recruitment assay at sub-micromolar concentrations. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd. AZD8797 selectively and with high affinity binds 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), with reduced potency for rat CX3CR1 (29 nM) and even lower for mouse CX3CR1 (54 nM).

Storage & Handling

Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CX3CR1, CXCR2, AZD 8797, AZD8797, AZD-8797, [125I]-CX3CL1-CX3CR1, 125I-IL-8-CXCR2, KAN-0440567, KAND567
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AZD8797

CAS: 911715-90-7

Key Properties

No computed properties available.

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AZD8797 (orb1707606)

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% DMSO +
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% Tween 80 +
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Available Sizes

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1 mg
$ 130.00
5 mg
$ 240.00
1 ml x 10 mM (in DMSO)
$ 260.00
10 mg
$ 340.00
25 mg
$ 560.00
50 mg
$ 770.00
100 mg
$ 1,030.00
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