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Cardiovascular Ion Channel Portfolio

Cardiovascular Ion Channel Profiling

Introduction

Control of smooth-muscle tension, which is essential for physiological regulation of vascular resistance, involves a wide range of ion channels. These include Ca2+-permeable channels such as Cav1.2, P2X4, nAChRα7, and many TRP channels, as well as channels that regulate vasoactive-substance release and arterial tone through control of membrane potential.

The latter group includes K+-selective channels such as BK, SK3, IK, Kir2.1, Kir6.1, Kir6.2, Kv1.5, and Kv7.1, together with the non-selective channel TRPM4.

Under pathological conditions including vascular inflammation, chronic hypertension, heart failure, and hypoxia, vascular integrity may decrease, endothelial permeability may increase, and hyperplasia may occur. Ion channels including Kv7.1, nAChRα7, and several TRP channels may contribute to these mechanisms and are therefore relevant to cardiovascular research.

PORTFOLIO SCOPE

Cardiovascular Ion Channel Portfolio

Our Cardiovascular Ion Channel Portfolio provides an off-target profile of principal ion channels that influence cardiovascular physiology.

The portfolio includes channels that may serve as therapeutic targets for hypertension, atherosclerosis, and heart failure. Because drug-induced dysfunction of these channels may contribute to adverse effects, systematic profiling supports cardiovascular safety assessment and mechanism-of-action research.

TARGET COVERAGE

Cardiovascular ion-channel assay panel

Ion Channel FamilyTargetMethodSpeciesMode
Voltage-gated sodium channelNav1.5Manual patch clamphumanAgonist or Antagonist
Voltage-gated potassium channelKv1.3Manual patch clamphumanAgonist or Antagonist
Kv1.5Manual patch clamphumanAgonist or Antagonist
hERG (Kv11.1)Manual patch clamphumanAgonist or Antagonist
Kv4.3Manual patch clamphumanAgonist or Antagonist
Iks (Kv7.1)Manual patch clamphumanAgonist or Antagonist
Potassium channel, calcium activatedBKManual patch clamphumanAgonist or Antagonist
IKManual patch clamphumanAgonist or Antagonist
Potassium channel, inward rectifierKir2.1Manual patch clamphumanAgonist or Antagonist
Kir3.1/3.4 (KAch, GIRK)Manual patch clamphumanAgonist or Antagonist
Kir6.2/Sur2AManual patch clamphumanAgonist or Antagonist
Voltage-gated calcium channelCav1.2Manual patch clamphumanAgonist or Antagonist
Cav3.2Manual patch clamphumanAgonist or Antagonist
Hyperpolarization-activated channelHCN2Manual patch clamphumanAgonist or Antagonist
HCN4Manual patch clamphumanAgonist or Antagonist
Transient receptor potential channelTRPA1Manual patch clamphumanAgonist or Antagonist
TRPV1Manual patch clamphumanAgonist or Antagonist
TRPV3Manual patch clamphumanAgonist or Antagonist
TRPV4Manual patch clamphumanAgonist or Antagonist
TRPM4Manual patch clamphumanAgonist or Antagonist
TRPM8Manual patch clamphumanAgonist or Antagonist
TRPC5Manual patch clamphumanAgonist or Antagonist
TRPC6Manual patch clamphumanAgonist or Antagonist
Ligand-gated ion channelP2X1Manual patch clamphumanAgonist or Antagonist
P2X4Manual patch clamphumanAgonist or Antagonist
P2X7Manual patch clamphumanAgonist or Antagonist
nAChR α7/RIC3Manual patch clamphumanAgonist or Antagonist

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