ABT-639  ≥98%(HPLC)

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沸点:612.2±65.0 °C(Predicted)
密度:1.51±0.1 g/cm3(Predicted)
包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介:ABT-639 是一种新型选择性的 T 型 Ca2+ 通道阻滞剂。
溶解性:溶于DMSO
储备液保存:-80°C, 2 years -20°C, 1 year
靶点:Ca2+ Channel
体外研究: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.
保存条件:-20°C
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