kca3.1

Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel that ameliorates RBC dehydration in the SAD mouse. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibits RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is used in the treatment of Sickle Cell Disease and Sickle Cell Anemia.

SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) is an activator of KCa3.1 and KCa2 channels (EC50s: 260, 2900, 2900 nM for KCa3.1, KCa2.1 and KCa2.2 respectively).

TRAM-34 (Triarylmethane-34) (Kd=20 nM), an effective and specific inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1), does not block cytochrome P450. The selective activity of TRAM-34(TRAM 34) is 200 to 1500-fold than other ion channels.

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK KCa2 and IK KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

OSK-1 is a potent potassium channel blocker belonging to the α-KTx3 toxins. It exhibits IC50 values of 0.6 nM, 5.4 nM, and 0.014 nM for Kv1.1, Kv1.2, and Kv1.3 channels, respectively. Additionally, OSK-1 acts as a moderate blocker of the calcium-activated KCa3.1 channel, with an IC50 of 225 nM. Consequently, OSK-1 finds application as an immunosuppressive drug.

High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

NS6180 is a potent and selective KCa3.1 channel inhibitor(IC50= 9 nM). It prevents T-cell activation and inflammation.

SKA-111 is a selective calcium-activated potassium phannel (potassium phannel ) KCa3.1 activator that induces membrane hyperpolarization in porcine endothelial cells.SKA-111 binds to the interface between the CaM N-valve and the S4-S5 junction and ameliorates Bradykinin-induced dilation of coronary arteries in the isolated rat heart, which can be used for the study of cardiovascular diseases. study of cardiovascular diseases.