AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.
体外研究
AZD8848 shows good activity against TLR7, with cellular pEC50s of 7.0 and 6.6 for human TLR7 and rat TLR7, respectively.
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.
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.
体内研究
AZD8848 (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.
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.
分子式
C29H43N7O5
分子量
569.70
CAS号
866269-28-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 25 mg/mL (43.88 mM; ultrasonic and warming and heat to 60°C)