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AZD8797
- Rugocrixan - CX3CR1 antagonist 18a - KAND567
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H25N5OS2
- MW: 403.56
Description
AZD8797 is a potent and selective Fractalkine receptor (CX3CR1) antagonist with a Ki value of 3.9 nM. AZD8797 exhibits 720-fold selectivity over CXCR2, 246-fold selectivity over CCR1, and 187-fold selectivity over CCR2, while showing no significant antagonism of CCR4, CCR5, CCR6, CXCR3, or CXCR5 receptors.
CX3CR1 is a chemokine receptor involved in leukocyte adhesion, migration, extravasation, and inflammatory responses. AZD8797 displays favorable metabolic stability, solubility, and high Caco-2 permeability, making it a valuable tool for investigating fractalkine signaling in inflammation, neuroinflammation, and immune cell trafficking. The only notable off-target activity identified was at the adenosine A1 receptor, where selectivity was determined to be 33-fold.
Key Features
- Potent CX3CR1 (Fractalkine receptor) antagonist
- Ki: 3.9 nM
- Highly selective over related chemokine receptors
- High Caco-2 permeability and favorable metabolic stability
- Useful tool for inflammation and immune cell migration research
Applications
- CX3CR1 and fractalkine signaling research
- Inflammation and neuroinflammation studies
- Leukocyte migration and adhesion research
- Immune cell trafficking investigations
- Multiple sclerosis and inflammatory disease models
More Information
| Parent CAS No. | 911715-90-7 |
|---|---|
| Chemical Name | (R)-2-(2-amino-5-((S)-1-phenylethylthio)thiazolo[4,5-d]pyrimidin-7-ylamino)-4-methylpentan-1-ol |
| SMILES | C(O)[C@H](NC1N=C(S[C@H](C2=CC=CC=C2)C)N=C2N=C(N)SC2=1)CC(C)C |&1:2,8,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C19H25N5OS2/c1-11(2)9-14(10-25)21-16-15-17(22-18(20)27-15)24-19(23-16)26-12(3)13-7-5-4-6-8-13/h4-8,11-12,14,25H,9-10H2,1-3H3,(H3,20,21,22,23,24)/t12-,14+/m0/s1 |
| InChiKey | ZMQSLMZOWVGBSM-GXTWGEPZSA-N |
| CID | 11965767 |
| Short Description | CX3CR1 antagonist |
References
- S. Karlström 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.
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