kir2.1

ML133 hydrochloride (ML133 HCl) is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.

Zacopride is a highly potent 5-HT3 receptor antagonist (Kd = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM). It also is a selective IK1 channel agonist.

VU591 hydrochloride is a selective renal outer medullary potassium channel (Kir1.1, ROMK) antagonist (IC50:0.24 μM). Thought to block the intracellular pore of the Kir1.1 channel. Exhibits no effect on Kir7.1 at concentrations up to 10 μM; does not inhibi

IK1 inhibitor PA-6 (PA-6) is a selective and potent inhibitor of IK1 (KIR2.x ion-channel-carried inward rectifier current) with an IC50 of 12-15 nM for human and mouse KIR2.x currents.

VU041 is an inhibitor of Anopheles gambiae and Aedes aegypti inward rectifier potassium 1 channels (IC50: 2.5 μM and 1.7 μM, respectively). VU041 inhibits appreciably is mammalian Kir2.1 (IC50: 12.7 μM) and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2 SUR1, and Kir7.1.

GPV0057 (Compound 5d) is a potent and selective inhibitor of P-glycoprotein (P-gp). It also acts as a selective activator of the potassium channel Kir2.1. By competitively binding at the substrate binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, thereby reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, enhancing potassium ion influx. GPV0057 has potential applications in the study of tumors with high P-gp expression and Kir2.1-related diseases, such as heart failure and Andersen-Tawil syndrome.

ML 297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML 297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters.

Lei-Dab7 TFA, a selective and high-affinity blocker of the K Ca 2.2 (SK2) channel with a dissociation constant (K d) of 3.8 nM, demonstrates over 200-fold selectivity for K Ca 2.2 compared to K Ca 2.1, K Ca 2.3, K Ca 3.1, K v, and Kir2.1. Furthermore, Lei-Dab7 TFA enhances theta-burst responses and long-term potentiation (LTP) in rat hippocampal slices in vitro.

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