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TTA-A2

CAS No. : 953778-63-7

MCE 站：TTA-A2

产品活性：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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: 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).

In Vivo: 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.

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