AZD8848 (C09-1103-160)

AZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitisIn VitroAZD8848 shows good activity against TLR7, with cellular pEC 50 s of 7.0 and 6.6 for human TLR7 and rat TLR7, respectively. AZD8848 has an EC 50 of 4 nM in the induction of IFNα from human PBMCs and an IC 50 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. AZD8848 is a potent, selective TLR7 agonist antedrug able to inhibit Th2 responses in vitro. AZD8848 has no activity against human TLR8 or against any of the other human TLRs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAZD8848 (0.1-1 mg/kg; intratracheal) has a good pharmacokinetics in the Brown Norway rat . AZD8848 (0.3 mg/kg; Intratracheal) suppresses the ovalbumin (OVA) challenge in the rat allergy model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Brown Norway rat allergy model Dosage: 0.1 mg/kg, 1 mg/kg Administration: Intratracheal (24 hours prior to and 24 hours after the OVA challenge) Result: Suppressed OVA challenge in a dose-dependent manner. Animal Model: Brown Norway rat Dosage: 0.3 mg/kg (Pharmacokinetic Analysis) Administration: Intratracheal Result: Has a very short half-life (0.2 min) in rat blood and declined slowly after this point and levels above 1000 nmol/kg were maintained for over 5 hours.IC50& Target:TLR7. Specifications and Purity: 10mM in DMSO. Molecular Formula: C29H43N7O5. Molecular Weight: 569.70.