TDI-10229 是一种有效的可口服生物可利用的可溶性腺苷酸环化酶 (sAC, ADCY10) 抑制剂。 TDI-10229 在生化(IC50 为 195 nM)和细胞测定(IC50 为 92nM)中均显示出纳摩尔级的 sAC 抑制作用,并表现出足以保证其用作体内工具化合物的小鼠药代动力学特性。
产品描述
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical (IC50 of 195 nM) and cellular assays (IC50 of 92nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound[1][2].
体外活性
TDI-10229 exhibits good permeability with an IC50 of 92 nM for human 4-4 cells[2].
体内活性
TDI-10229 (20 mg/kg; p.o.) treatment shows the Cmax, AUC and MRT were 15.5 μM, 94 μg h/mL and 3.95 hours, respectively[2].
Cas No.
T9613
分子式
C16H16ClN5
分子量
313.79
储存和溶解度
DMSO:125 mg/mL (398.37 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years