PDE4B-IN-2 是一种具有口服活性,选择性 PDE4B 抑制剂,IC50 为 15 nM。PDE4B-IN-2 抑制 PDE4D (IC50=1.7 μM)。PDE4B-IN-2 表现出有效的抗炎作用。
产品描述
PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 μM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.
体外活性
PDE4B-IN-2 (compound 33) does not inhibit CYP1A2, CYP3A4, CYP2C9, and CYP2D (IC50>10 μM). PDE4B-IN-2 inhibits LPS-induced TNF-aproduction in vitro from mouseperipheral blood mononuclear cell (PBMC; IC50=0.5 M)[1].
体内活性
PDE4B-IN-2 (compound 33; 2 mg/kg; po) has a Cmax of 8.7 μg/mL and an AUC of 52.3 μgoh/mL in mice[1].
Cas No.
915082-52-9
分子式
C19H18ClN3O2S
分子量
387.88
别名
A 33
储存和溶解度
DMSO:22.5mg/mL (58mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years