TTA-A2 - CAS:953778-63-7

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TTA-A2

目录号 : KM8918 CAS No. : 953778-63-7 纯度 : 98%

Data Sheet 产品使用指南

TTA-A2 是一种强效、选择性和口服活性的 T 型电压门控钙通道 (calcium channel) 拮抗剂，可减少孕烷 X 受体 (PXR) 的激活。TTA-A2 对 Cav3.1 (a₁G) 和 Cav3.2 (a₁H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC₅₀ 值分别为 89 nM 和 92 nM。TTA-A2 可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。

规格	价格	是否有货
1mg		In-stock
5mg	询价	In-stock
10mg	询价	In-stock

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生物活性

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.

体外研究

TTA-A2 exhibits a state-dependent inhibition of α₁I with potencies of 98 nM and 3.7 μM at membrane holding potentials of -80 and -100 mV, respectively in astandard voltage-clamp electrophysiology assay. It also exhibits excellent selectivity against the Cav1.2 (L-type), Cav2.1 (P/Q-type), Cav2.2 (N-type), and Cav2.3 (R-type) channels which all had IC₅₀ values of >30 μM at 80 mV.
TTA-A2 exhibits high affinity in the α₁I binding assay with a K_i of 1.2 nM and has excellent selectivity over the hERG potassium channel and L-type calcium channel (both IC₅₀>10 μM).

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.

分子式

C₂₀H₂₁N₂O₂F₃

分子量

378.39

CAS号

953778-63-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (264.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6428 mL	13.2139 mL	26.4278 mL
5 mM	0.5286 mL	2.6428 mL	5.2856 mL
10 mM	0.2643 mL	1.3214 mL	2.6428 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.61 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.61 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。