AZD8848 是一种选择性的 TLR7 前体药激动剂，用于哮喘和过敏性鼻炎的研究。
AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug 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].
[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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