1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. TTA-A2

TTA-A2 

目录号: HY-111828 纯度: >99.0%
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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。

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TTA-A2 Chemical Structure

TTA-A2 Chemical Structure

CAS No. : 953778-63-7

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Description

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[1][2].

IC50 & Target

IC50: 98 nM ( α1I at membrane holding potentials of -80 mV)
IC50: 3.7 μM (α1I at membrane holding potentials of -100 mV)[1]

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[1].
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)[1].

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[1].
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[2].

Animal Model: Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mices[2]
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.
Molecular Weight

378.39

Formula

C₂₀H₂₁F₃N₂O₂

CAS No.

953778-63-7

SMILES

O=C(N[C@@H](C1=NC=C(OCC(F)(F)F)C=C1)C)CC2=CC=C(C3CC3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >99.0%

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Keywords:

TTA-A2Calcium ChannelCa2+ channelsCa channelsT-type calcium channelPregnane X receptorElectrocorticogramEpilepsyneurological diseasessleep disordersInhibitorinhibitorinhibit

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TTA-A2
目录号:
HY-111828
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