cav1.2

Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.

AT1R antagonist 3 (Compound 1) is an antagonist of the angiotensin II type 1 receptor (AT1R) and an inhibitor of the L-type calcium channel CaV1.2 (IC50=0.57 μM). It exhibits vasodilatory effects in isolated rat aorta (10 μM, 88.7%) and shows antihypertensive activity in rat models.

DPP8/9-IN-2 (Compound 21) is an inhibitor targeting DPP8 and DPP9 with IC50 values of 0.22 nM and 3 nM, and Ki values of 2.9 nM and 6 nM, respectively. It exhibits certain cardiac toxicity, with IC50 values against the hERG potassium channel, Nav1.5 sodium channel, and Cav1.2 calcium channel of 0.7 μM, 29.0 μM, and 27.7 μM. DPP8/9-IN-2 is applicable for research into diseases such as cancer.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

Onychocin B is a cyclic tetrapeptide isolated from Onychocola sclerotica. It functions as a calcium channel blocker with an IC50 value of 7.1 μM for Cav1.2.

Ambocin is a natural product from Pueraria mirifica. Ambocin blocks Ba2+ currents through CaV1.2 channels (IBa1.2) in a concentration-dependent manner and increases IKCa1.1.