货号	规格	价格	上海	北京	珠海	重庆	武汉
S88235-5mg	≥98%	￥1200.00 S88235-5mg ￥1200.00 3-5天	0 货期：3-5天	-	-	-	-
S88235-10mg	≥98%	￥2000.00 S88235-10mg ￥2000.00 3-5天	0 货期：3-5天	-	-	-	-
S88235-25mg	≥98%	￥2900.00 S88235-25mg ￥2900.00 3-5天	0 货期：3-5天	-	-	-	-
S88235-50mg	≥98%	￥5500.00 S88235-50mg ￥5500.00 3-5天	0 货期：3-5天	-	-	-	-

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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。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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分子摩尔量

计算重置

(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide