AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.
IC50&Target
TLR7
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)