2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. ABT-639 hydrochloride

ABT-639 hydrochloride 是一种新型选择性的 T 型 Ca2+ 通道阻滞剂。

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ABT-639 hydrochloride Chemical Structure

ABT-639 hydrochloride Chemical Structure

CAS No. : 1235560-31-2

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ABT-639 hydrochloride 的其他形式现货产品:

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ABT-639 hydrochloride 相关抗体

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

IC50 & Target

Ca2+ Channel[1]
体内研究
(In Vivo)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

492.37

Formula

C20H21Cl2F2N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration
[1]

Rats[1]
The pharmacokinetic properties are determined in Sprague Dawley rats dosed intravenously with 5 μmol/kg ABT-639 prepared in 10% DMSO/90% poly ethylene glycol 400 (PEG400). The plasma levels of ABT-639 are determined using HPLC and mass spectrometry. Following oral administration (p.o.) of the ABT-639 (3, 10 and 30 mg/kg) prepared in 10% PEG400/10% Cremophor EL/80% Oleic Acid the levels of ABT-639 in plasma and brain are determined. Briefly, the brains are immediately removed and freed from blood vessels as much as possible. The resulting brain tissues are frozen at -20°C, followed by weighing and homogenization before analysis. The heparinized blood samples are also frozen (-20°C) until analysis. ABT-639 is separated from the blood and brain samples using protein precipitation with acetonitrile followed by quantification with liquid chromatography/mass spectroscopy. Plasma samples for concentration determinations from in vivo efficacy experiments are collected from each animal within 15 min following behavioral testing.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

ABT-639 hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

ABT-6391235560-31-2ABT639ABT 639Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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产品名称：
ABT-639 hydrochloride
目录号：
HY-101616
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