ABT-639 是一种有效的选择性 T 型钙通道阻滞剂。

ABT-639 is a potent and selective T-type calcium channel blocker.

ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50 >30 μM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.

Following oral administration ABT-639 produces dose-dependent antinociception in a rat model of knee joint pain (ED50 = 2 mg/kg, p.o.). ABT-639 (10-100 mg/kg, p.o.) also increases tactile allodynia thresholds in multiple models of neuropathic pain. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states.

1235560-28-7

C20H20ClF2N3O3S

455.9

ABT 639;ABT-639

DMSO:≤10 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years