A CX3CR1 antagonist
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AZD 8797

Item No. 28419

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-2-[[2-amino-5-[[(1S)-1-phenylethyl]thio]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methyl-1-pentanol
CAS Number
911715-90-7
Molecular Formula
C19H25N5OS2
Formula Weight
403.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
246 nm
SMILES
NC1=NC2=NC(S[C@@H](C)C3=CC=CC=C3)=NC(N[C@@H](CO)CC(C)C)=C2S1
InChi Code
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
InChi Key
ZMQSLMZOWVGBSM-GXTWGEPZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $74

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    5 mg

    $252

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    10 mg

    $440

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    Product Description

    AZD 8797 is a chemokine (C-X3-C motif) receptor 1 (CX3CR1) antagonist (Ki = 3.9 nM). It is selective for CX3CR1 over CX3CR2 (Ki = 2,800 nM).1 AZD 8797 (0.1-10 µM) inhibits [35S]GTPγS accumulation induced by chemokine (C-X3-C) ligand 1 (CX3CL1) in CHO cell membranes expressing human CX3CR1.2 It inhibits adhesion of RBMI-8226 cells to CX3CL1 (IC50 = 5.8 nM). AZD 8797 (39 and 78 µmol/kg per day) reduces spinal cord inflammation and demyelination, as well as the incidence of disease relapse, in a rat model of myelin oligodendrocyte glycoprotein-induced experimental autoimmune encephalomyelitis (EAE).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shima, H., Matsumoto, M., Ishigami, Y., et al. S-Adenosylmethionine synthesis is regulated by selective N6-adenosine methylation and mRNA degradation involving METTL16 and YTHDC1. Cell Rep. 21(12), 3354-3363 (2017).

    2. Cederblad, L., Rosengren, B., Ryberg, E., et al. AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor. Biochem. J. 473(5), 641-649 (2016).

    3. Wollberg, A.R., Ericsson-Dahlstrand, A., Jureus, A., et al. Pharmacological inhibition of the chemokine receptor CX3CR1 attenuates disease in a chronic-relapsing rat model for multiple sclerosis. PNAS 111(14), 5409-5414 (2014).