产品信息
抗原名称
Calcium Channel
商品描述
ABT-639是一种新型的, 外周起作用的, 选择性T型钙通道阻滞剂, 阻断人T型 (Cav3.2) Ca 2+通道中 (IC50 =2μM) 和降低大鼠DRG神经元LVA电流 (IC50 =8μM)。
分子量
455.91
纯度
98%
可溶性
DMSO : 10 mg/mL (21.93 mM; Need ultrasonic and warming)
外观
Powder
In vivo(体内研究)
ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 μM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 μM). ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50>30 mM). 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 (e.g. spinal nerve ligation, CCI, and vincristine-induced, and capsaicin secondary hypersensitivity). ABT-639 does not attenuate hyperalgesia in inflammatory pain models induced by complete Freund’s adjuvant or carrageenan. At higher doses (e.g. 100-300 mg/kg) ABT-639 does not significantly alter hemodynamic or psychomotor function. The antinociceptive profile of ABT-639 provides novel insights into the role of peripheral T-type (Cav3.2) channels in chronic pain states.
背景
别名
ABT-639; ABT 639
分子式
C20H20ClF2N3O3S
CAS号
1235560-28-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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