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。

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 (a 1 G) and Cav3.2 (a 1 H) channels with IC 50 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.

Solid

IC50: 98 nM ( α1I at membrane holding potentials of -80 mV)
IC50: 3.7 μM (α1I at membrane holding potentials of -100 mV)

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 Ki of 1.2 nM and has excellent selectivity over the hERG potassium channel and L-type calcium channel (both IC50>10 μM).
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

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

[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.

In Vitro: DMSO : 100 mg/mL (264.28 mM; Need ultrasonic)配制储备液