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Cardiovascular Ion Channel Portfolio

Introduction

The control of smooth muscle tension, which is essential for physiological regulation of vascular resistance, involves a variety of ion channels. These channels include Ca2+-permeable channels such as Cav1.2, P2X4, nAChRα7, and most TRP channels. Additionally, there are channels that regulate the release of vasoactive substances and those that control arterial tone by managing membrane potential. The latter group includes K+-selective channels like BK, SK3, IK, Kir2.1, Kir6.1, Kir6.2, Kv1.5, and Kv7.1, as well as the non-selective channel TRPM4.

Under pathological conditions such as vascular inflammation, chronic hypertension, heart failure, or hypoxia, the vascular integrity may decrease, endothelial permeability may increase, and hyperplasia may occur, all of which can compromise vascular function. Certain ion channels play a role in these pathological mechanisms, including Kv7.1, nAChRα7, and several TRP channels.

 

Cardiovascular Ion Channel Portfolio

Our cardiac portfolio offers a comprehensive off-target profile of the principal ion channels that have an impact on physiological function of Cardiovascular system.

Recognizing the significance of these channels, our Cardiovascular Ion Channel Portfolio has been designed to include a selection of channels that are potential therapeutic targets for conditions like hypertension, atherosclerosis, and heart failure. It is important to note that dysfunction of these channels, potentially induced by drugs, may lead to adverse effects. This highlights the importance of understanding and profiling ion channels in the context of cardiovascular health and disease


Protein Assay Table

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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