S82525 |
ABT-639 |
源叶(MedMol) | 99% |
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- 产品描述: ABT-639 is a potent and selective T-type calcium channel blocker.
- 靶点: Calcium Channel;CalciumChannel
- 体外研究:
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.
- 体内研究:
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.
- 参考文献:
1. Jarvis MF, et al. A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats. Biochem Pharmacol. 2014 Jun 15;89(4):536-44.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.193 ml 10.967 ml 21.934 ml 5 mM 0.439 ml 2.193 ml 4.387 ml 10 mM 0.219 ml 1.097 ml 2.193 ml 50 mM 0.044 ml 0.219 ml 0.439 ml
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