
AZD8797
CAS No. 911715-90-7
AZD8797( —— )
Catalog No. M33276 CAS No. 911715-90-7
AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 126 | Get Quote |
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5MG | 188 | Get Quote |
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10MG | 353 | Get Quote |
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25MG | 725 | Get Quote |
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50MG | 908 | Get Quote |
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100MG | 1287 | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameAZD8797
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NoteResearch use only, not for human use.
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Brief DescriptionAZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2.
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DescriptionAZD8797 (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.
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In VitroIn 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. 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).
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In VivoAZD8797 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.
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Synonyms——
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PathwayAutophagy
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TargetCXCR
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RecptorCXCR
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Research Area——
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Indication——
Chemical Information
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CAS Number911715-90-7
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Formula Weight403.56
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Molecular FormulaC19H25N5OS2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 150 mg/mL (371.69 mM )
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SMILESCC(C)C[C@H](CO)Nc1nc(S[C@@H](C)c2ccccc2)nc2nc(N)sc12
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Cederblad L, et al. AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor. Biochem J. 2016 Mar 1;473(5):641-9.?
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