產(chǎn)品名稱(chēng)

AZD 8797 - CX3CR1 antagonist 18a

產(chǎn)品貨號(hào)

Axon 2255 CAS [911715-90-7] MF C19H25N5OS2MW 403.56 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Potent and selective antagonist of the Fractalkine receptor (FKN or CX3CR1; Ki value 3.9 nM) with a 720 fold selectivity over the CXCR2 receptor, a 246-fold selectivity versus hCCR1 and 187-fold versus hCCR2 and no significant antagonism of the CCR4, CCR5, CCR6, CXCR3, and CXCR5 receptors.?AZD 8797 displayed adequate metabolic stability and solubility and high Caco-2 permeability. Notably, AZD 8797 exhibited a significant interaction (>50% activity at 10 μM) for the adenosine A1 receptor only, and the selectivity was later determined to be 33-fold.? KEYWORDS:

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axonmedchem

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AZD 8797 - CX3CR1 antagonist 18a

Based on 4 publications in PubMed 10 10 4

Axon 2255

CAS [911715-90-7]

MF C19H25N5OS2
MW 403.56

Purity: 99%
Optical purity: Optically pure
Soluble in DMSO

AZD 8797

Description

Potent and selective antagonist of the Fractalkine receptor (FKN or CX3CR1; Ki value 3.9 nM) with a 720 fold selectivity over the CXCR2 receptor, a 246-fold selectivity versus hCCR1 and 187-fold versus hCCR2 and no significant antagonism of the CCR4, CCR5, CCR6, CXCR3, and CXCR5 receptors.?
AZD 8797 displayed adequate metabolic stability and solubility and high Caco-2 permeability.
Notably, AZD 8797 exhibited a significant interaction (>50% activity at 10 μM) for the adenosine A1 receptor only, and the selectivity was later determined to be 33-fold.?

S. Karlstr?m 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, 56, 3177-3190.?

L Cederblad et al. AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor. Biochem J. 2016 Mar 1;473(5):641-9.

A Ridderstad Wollberg 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.

Certificate of Analysis
Material Safety Data Sheet

Cell Signaling & Oncology CNS Immunology Pain & Inflammation A1 Chemokine

Potent and selective antagonist of the Fractalkine receptor (FKN or CX3CR1)

Chemical name

(R)-2-(2-amino-5-((S)-1-phenylethylthio)thiazolo[4,5-d]pyrimidin-7-ylamino)-4-methylpentan-1-ol

Parent CAS No.

[911715-90-7]

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