AZD8848

• CAT Number: I003849
• CAS Number: 866269-28-5
• Molecular Formula: C29H43N7O5
• Molecular Weight: 569.70
• Purity: ≥95%
• Synonyms: methyl 2-[3-[[3-(6-amino-2-butoxy-8-oxo-7H-purin-9-yl)propyl-(3-morpholin-4-ylpropyl)amino]methyl]phenyl]acetate
• InChI: InChI=1S/C29H43N7O5/c1-3-4-16-41-28-32-26(30)25-27(33-28)36(29(38)31-25)13-7-12-35(11-6-10-34-14-17-40-18-15-34)21-23-9-5-8-22(19-23)20-24(37)39-2/h5,8-9,19H,3-4,6-7,10-18,20-21H2,1-2H3,(H,31,38)(H2,30,32,33)
• InChIKey: FEFIBEHSXLKJGI-UHFFFAOYSA-N
• SMILES: CCCCOC1=NC(=C2C(=N1)N(C(=O)N2)CCCN(CCCN3CCOCC3)CC4=CC=CC(=C4)CC(=O)OC)N

AZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitis[1].
AZD8848 shows good activity against TLR7, with cellular pEC50s of 7.0 and 6.6 for human TLR7 and rat TLR7, respectively[1].
AZD8848 has an EC50 of 4 nM in the induction of IFNα from human PBMCs and an IC50 of 0.2-1.0 nM for the inhibition of IL-5, irrespective of whether the T cells have been polyclonally stimulated with PHA or via antigen presentation[1].
AZD8848 is a potent, selective TLR7 agonist antedrug able to inhibit Th2 responses in vitro[1].
AZD8848 has no activity against human TLR8 or against any of the other human TLRs[1].
AZD8848 (0.1-1 mg/kg; intratracheal) has a good pharmacokinetics in the Brown Norway rat[1].
AZD8848 (0.3 mg/kg; Intratracheal) suppresses the ovalbumin (OVA) challenge in the rat allergy model[1].

Reference

[1]. Delaney S, et al. Tolerability in man following inhalation dosing of the selective TLR7 agonist, AZD8848. BMJ Open Respir Res. 2016 Feb 23;3(1):e000113.
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