TTA-A2

A T-type calcium channel inhibitor (IC50s = 89, 92, and 98 nM for Cav3.1, Cav3.2, and Cav3.3, respectively, in patch-clamp assays at -80 mV), selective for these channels over Cav1.2, Cav2.1, Cav2.2, and Cav2.3 in patch-clamp assays (IC50s = >30 µM for all at -90 mV), reduces the viability of spheroid A549 lung cancer cells at 100 or 200 nM, decreases body weight gain and fat mass and increases lean muscle mass in mice fed a high-fat diet, inhibits amphetamine- or MK-801-induced locomotor activity in rats at 3 mg/kg, decreases the mean time spent in active wake and REM sleep and increases the mean time spent in delta sleep in wild-type but not Cacna1g-/- and Cacna1i-/- double knockout mice when administered one hour before the inactive phase at 10 mg/kg. Formulation: A solid. InChI: InChI=1S/C20H21F3N2O2/c1-13(18-9-8-17(11-24-18)27-12-20(21,22)23)25-19(26)10-14-2-4-15(5-3-14)16-6-7-16/h2-5,8-9,11,13,16H,6-7,10,12H2,1H3,(H,25,26)/t13-/m1/s1. InChIKey: GEYDMBNDOVPFJL-CYBMUJFWSA-N. SMILES: O=C(CC1=CC=C(C2CC2)C=C1)N[C@H](C)C3=CC=C(OCC(F)(F)F)C=N3