TTA-A2

**TTA-A2** is a highly selective, potent small molecule antagonist of T-type calcium channels (Ca(v)3.1, Ca(v)3.2, Ca(v)3.3) with voltage-dependent inhibition and strong selectivity (IC50 ∼100 nM, ∼300-fold selectivity vs. high-voltage activated calcium channels)[1][4]. It acts by stabilizing the inactivated state of the channel, causing a hyperpolarized shift in channel availability and delaying recovery from inactivation. TTA-A2 suppresses wakefulness and promotes slow-wave sleep in animal models, showing utility in neurological disorders such as sleep disorders and epilepsy[1][4]. In cancer research, TTA-A2 reduces chemoresistance and enhances the effects of chemotherapeutic agents such as paclitaxel, possibly by inhibiting calcium influx and downregulating T-type channel expression[2][3][7]. Its potential indications include sleep disorders, epilepsy, and cancer (as an adjuvant in chemotherapy).

Other names

2-(4-cyclopropylphenyl)-N-((1R)-1-{5-[(2,2,2-trifluoroethyl)oxo]-pyridin-2-yl}ethyl)acetamide