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(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide
S88235 |
(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide |
源叶(MedMol) | 98% |
- 产品描述: TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy
- 靶点: IC50: 98 nM ( α1I at membrane holding potentials of -80 mV) IC50: 3.7 μM (α1I at membrane holding potentials of -100 mV);CalciumChannel
- 体内研究:
TTA-A2 (oral gavage; 3 mg/kg; single dose) produces significant changes in sleep architecture in rats. A reduction in active wake soon after dosing with a concurrent increase in delta sleep and decrease in REM sleep. Additionally, these effects persists for up to 4 h post-dose in rats. TTA-A2 (oral gavage; 10 mg/kg; once daily; 5 days) shows selective effect on recurrent thalamocortical network activity, it suppresses active wake and promotes slow-wave sleep in wild-type mice but not in mice lacking both Cav3.1 and Cav3.3. Animal Model: Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mices Dosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg; once daily; 5 days Result: Blocked active wake and promotes slow-wave sleep in wild-type mice but not mutant mice.
- 参考文献:
1. Thomas S Reger, et al.Pyridyl amides as potent inhibitors of T-type 2. Richard L Kraus, et al.In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice. J Pharmacol Exp Ther. 2010 Nov;335(2):409-17.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.643 ml 13.214 ml 26.428 ml 5 mM 0.529 ml 2.643 ml 5.286 ml 10 mM 0.264 ml 1.321 ml 2.643 ml 50 mM 0.053 ml 0.264 ml 0.529 ml
- 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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