TTA-A2 is a potent, selective, and orally active T-type voltage-gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. It 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 various human neurological diseases, including sleep disorders and epilepsy.
- Potent, selective, orally active T-type voltage-gated calcium channel antagonist.
- Reduced pregnane X receptor (PXR) activation.
- Equally potent against Cav3.1 and Cav3.2 channels.
- Used in research for neurological diseases, sleep disorders, and epilepsy.
- Exhibits high affinity in α1I binding assay (Ki of 1.2 nM).
- Excellent selectivity over hERG potassium and L-type calcium channels.
- Modifies sleep architecture in rats and mice.