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AZD8797

Catalog No. T14384 CAS 911715-90-7

Synonyms: KAN-0440567, KAND567

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

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AZD8797, CAS 911715-90-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 83.00
5 mg	In stock	$ 198.00
10 mg	In stock	$ 372.00
25 mg	In stock	$ 788.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,430.00
1 mL * 10 mM (in DMSO)	In stock	$ 228.00

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Purity: 99.68%

Purity: 98.73%

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Description	AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.
Targets&IC50	[125I]-IL8-CXCR2:2800 nM (Ki, HEK293S cells), [125I]-CX3CL1-CX3CR1:3.9 nM (Ki, HEK293S cells), CX3CR1 (human):4 nM (Ki), CX3CR1:10 nM (human), B-lymphocyte cell lines:6 nM, CX3CR1 (rat):7 nM (Ki), CX3CR1:29 nM (Rat), CX3CR1:54 nM (mouse), WB (human):300 nM
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. In a β-arrestin recruitment assay, AZD8797 positively modulates the CX3CL1 response at sub-micromolar concentrations. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd[1]. 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). The potency is threefold lower for rat CX3CR1 (29 nM) and decreases even further at mouse CX3CR1 (54 nM)[3].
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[3].

Synonyms	KAN-0440567, KAND567
Molecular Weight	403.56
Formula	C19H25N5OS2
CAS No.	911715-90-7

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (247.79 mM)

References and Literature

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. 2. Sofia Karlströ, et al. Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1). J Med Chem. 2013 Apr 25;56(8):3177-90. 3. Ridderstad Wollberg A, et al. Pharmacological inhibition of the chemokine receptor CX3CR1 attenuates disease in a chronic-relapsing rat model for multiple sclerosis. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5409-14.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library

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Keywords

AZD8797 911715-90-7 Autophagy GPCR/G Protein Immunology/Inflammation CXCR KAN-0440567 AZD 8797 KAND567 AZD-8797 inhibitor inhibit

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