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Ion Channel Screening & Profiling Services

IntroductionServices OverviewComprehensive Ion ChannelsCase Study

Brief Introduction

Ion channels are pore-forming membrane proteins that create a gated, water-filled pore to help establish and control voltage potential across cell membranes through control of the active flow of ions between the intracellular and the extracellular environments. As key components in a wide variety of biological processes involved in rapid changes in cells (e.g. cardiac/skeletal/smooth muscle contraction, and epithelial transport of nutrients), ion channels are important therapeutic targets in a range of indications, including cardiac, CNS, immune system and metabolic diseases. Due to the development of screening technologies, a dramatically increased interest has been shown in ion channels for hit validation, potency determination, selectivity profiling and lead optimization.

Figure. 1 The structure of ion channels.Figure. 1 The structure of ion channels.

Creative Biogene's Service Highlights

With over ten years in ion channel research, Creative Biogene understands client needs and works closely to reduce experimental risk, optimize assays, and deliver high-quality, reproducible data.

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High-Throughput Ion Channel Screening

Creative Biogene's platforms allow rapid assessment of potency, efficacy, selectivity, and potential off-target effects. Both off-the-shelf and fully customized assays are available, covering major cardiac, CNS, and PNS channels. This approach enables early identification of promising leads while minimizing time and resource investment.

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Flexible and Customizable Assays

Our ion channel services are designed to meet diverse project requirements, from high-throughput screening to lead optimization. Clients can select individual channels or design multi-channel panels tailored to their targets of interest. Customized assay conditions, including concentration ranges, stimulation protocols, and detection methods, can be incorporated to align with specific research goals.

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Integrated Ion Channel Solutions

In addition to assay services, Creative Biogene offers a broad range of ion channel-related reagents and tools, including stable cell lines, premade viral particles, cell lysates, cloned constructs, and RNAi products. These resources provide a complete toolkit to support target validation, mechanistic studies, and preclinical development.

Broad-Spectrum Ion Channel Screening & Profiling

Ligand Gated Ion Channels

Creative Biogene provides a wide range of ligand-gated ion channels, including GABAA, P2X, nAChR, NMDA, and AMPA. Assays using manual patch clamp, Qpatch, FLIPR, and TEVC allow precise evaluation of activity, selectivity, and modulation, supporting hit identification and lead optimization.

GABA

P2XR

nAChR

NMDA

AMPA

ChannelOfficial SymbolMethod
GABAA(α1β2γ2)GABRA1/GABRB2/GABRG2Manual, Qpatch
GABAA(α1β3γ2)GABRA1/GABRB3/GABRG2Manual
GABAA(α2β2γ2)GABRA2/GABRB2/GABRG2Manual
GABAA(α2β3γ2)GABRA2/GABRB3/GABRG2Manual
GABAA(α3β2γ2)GABRA3/GABRB2/GABRG2Manual
GABAA(α3β3γ2)GABRA3/GABRB3/GABRG2Manual
GABAA(α4β3γ2)GABRA4/GABRB3/GABRG2Manual
GABAA(α4β3γ2)GABRA4/GABRB3/GABRG2Manual
GABAA(α4β3δ)GABRA4/GABRB3/GABRDManual
GABAA(α5β2γ2)GABRA5/GABRB2/GABRG2Manual
GABAA(α5β3γ2)GABRA5/GABRB3/GABRG2Manual
GABAA(α6β2γ2)GABRA6/GABRB2/GABRG2Manual
GABAA(α6β3δ)GABRA6/GABRB3/GABRDManual
ChannelOfficial SymbolMethod
hP2X1P2RX1Manual
hP2X3P2RX3Manual, Qpatch, FLIPR
rP2X3P2rx3Manual, FLIPR
gpP2X3P2rx3Manual
hP2X2/3P2RX2/P2RX3Manual, Qpatch, FLIPR
rP2X2/3P2rx2/P2rx3Manual, FLIPR
gpP2X2/3P2rx2/P2rx3Manual
hP2X4P2RX4Manual
hP2X5P2RX5Manual
hP2X7P2RX7Manual, FLIPR
ChannelOfficial SymbolMethod
nAChR-α3β4CHRNA3/CHRNB4TEVC bipolar
nAChR-α4β2CHRNA4/CHRNB2Manual, Qpatch, FLIPR
nAChR-α7/RIC3CHRNA7/αRIC3Manual, Qpatch, FLIPR
nAchRα1CHRNA1Activation or inhibition
nAchRα1CHRNA1Activation or inhibition, pre-incubation with nAch
nAChR-α7CHRNA7Activation or inhibition
nAChR-α7CHRNA7Activation or inhibition, pre-incubation with nAch
nAChR-α4β2CHRNA4/CHRNB2Activation or inhibition
nAChR-α4β2CHRNA4/CHRNB2Activation or inhibition, pre-incubation with nAch
nAChR(α1)2β1εδCHRNA1/CHRNB1/CHRNE/CHRNDActivation or inhibition
nAChR(α1)2β1εδCHRNA1/CHRNB1/CHRNE/CHRNDActivation or inhibition, pre-incubation with nAch
ChannelOfficial SymbolMethod
rNR1/NR2AGrin1/Grin2aManual
hNR1/NR2AGRIN1/GRIN2AManual
hNR1/NR2BGRIN1/GRIN2BManual, TEVC bipolar
rNR1/NR2BGrin1/Grin2bManual
hNR1/NR2CGRIN1/GRIN2CManual
hNR1/NR2DGRIN1/GRIN2DManual
ChannelOfficial SymbolMethod
AMPAGRIA1Manual

Voltage Gated Ion Channels (VGIC)

Our VGIC panel covers sodium, potassium, calcium channels, TRP, HCN, CRAC, and chloride channels. Flexible platforms enable single or multi-channel testing with customizable protocols, supporting HTS, lead optimization, and safety studies.

Sodium

Potassium

Calcium

TRP

HCN

Chloride

ChannelOfficial SymbolMethod
NaV1.1SCN1AManual, Qpatch
NaV1.2SCN2AManual, Qpatch
NaV1.3SCN3AManual, Qpatch
NaV1.4SCN4AManual, Qpatch
NaV1.5SCN5AManual, Qpatch
NaV1.6SCN8AManual
NaV1.7SCN9AManual, Qpatch in optimization
rNaV1.7SCN9AManual
NaV1.8SCN10AManual
rNaV1.8SCN10AManual
Late NaSCN5AManual
ChannelOfficial SymbolMethod
SK1KCNN1Manual
SK2KCNN2Manual
SK3KCNN3Manual
BKα1β1KCNMB1Manual
BKα1β4KCNMB4Manual
IK1/IKCaKCNN4Manual
hERG/Kv11.1KCNH2Manual, Qpatch, FLIPR
KCNQ1/Kv7.1KCNQ1 /KCNE1Manual, Qpatch in optimization
KCNQ2/Kv7.2KCNQ2Manual
KCNQ3/Kv7.3KCNQ3Manual
KCNQ4/Kv7.4KCNQ4Manual
KCNQ5/Kv7.5KCNQ5Manual
KCNQ2/3KCNQ2/KCNQ3Manual, Qpatch
KCNQ2/4KCNQ2/KCNQ4Manual
KCNQ3/5KCNQ3/KCNQ5Manual
Kir2.1KCNJ2Manual
Kir3.1/3.4KCNJ3/KCNJ5Manual
Kir3.2KCNC2Manual
Kir4.1KCNJ10Qpatch to be optimized, FLIPR
Kir6.2/SUR2AKCNJ11/ABCC9Manual
Kir6.2/SUR1KCNJ11/ABCC8Manual
TREK1KCNK2Manual
TASK1KCNK3Manual
TASK2KCNK5Manual
Kv1.1KCNA1Manual
Kv1.2KCNA2Manual
Kv1.3KCNA3Manual, Qpatch
Kv1.4KCNA4Manual
Kv1.5KCNA5Manual
Kv1.6KCNA6Manual
Kv1.7KCNA7Manual
Kv2.1KCNB1Manual
Kv2.2KCNB2Manual
Kv3.1KCNC1Manual
Kv3.2KCNC2Manual
Kv3.4KCNC4Manual
Kv4.2/KChIP2.2KCND2/KCNIP2Manual, Qpatch in optimization
Kv4.3KCND3Manual, Qpatch in optimization
ChannelOfficial SymbolMethod
CaV1.1CACNA1S/CACNB2/CACNA2DManual
CaV1.2 (L-type)CACNA1C/CACNB2/CACNA2D1Manual, Qpatch in optimization
CaV1.3CACNA1D/CACNB3/CACNA2DManual
CaV1.4CACNA1F/CACNB2/CACNA2DManual
CaV2.1 (P/Q-type)CACNA1A/CACNB4/CACNA2D1Manual
CaV2.2 (N-type)CACNA1B/CACNB3/CACNA2D1Manual, Qpatch & FLIPR in optimization
CaV2.3CACNA1E/CACNB3/CACNA2DManual
CaV3.1CACNA1GManual
CaV3.2 (T-type)CACNA1HManual
CaV3.3CACNA1IManual
CRAC (STIM1/Orai)STIM1/OraiManual
ChannelOfficial SymbolMethod
TRPA1TRPA1Manual, FLIPR
TRPC1TRPC1Manual
TRPC5TRPC5Manual
TRPC6TRPC6Manual, FLIPR
TRPC7TRPC7Manual
TRPM3TRPM3Manual
TRPM4/SUR1TRPM4/ABCC8Manual
TRPM8TRPM8Manual, FLIPR
TRPML1TRPML1Manual
TRPML3TRPML3Manual
TRPV1TRPV1Manual, FLIPR
TRPV2TRPV2Manual
TRPV3TRPV3Manual
TRPV4TRPV4Manual, FLIPR
TPC2TPCN2Manual
ChannelOfficial SymbolMethod
HCN1HCN1Manual
HCN2HCN2Manual
HCN3HCN3Manual
HCN4HCN4Manual
ChannelOfficial SymbolMethod
CFTRCFTRManual, TEVC bipolar
TMEM16AANO-1Manual
TMEM16BANO-2Manual
CLCN1CLCN1Manual

Others

We also provide assays for other important channels, including 5-HT3A, ASICs, and GlyR. Multiple assay formats deliver reliable, reproducible data to accelerate target validation and screening.

ChannelOfficial SymbolMethod
5-HT3AHTR3AManual, Qpatch, FLIPR, TEVC bipolar
ASIC1aASIC1Manual
ASIC1bASIC1Manual
ASIC3ASIC3Manual
GlyRα1/βGLRA1/GLRBManual

Case Study

The research team aimed to investigate the effects of a chemically modified α-cobratoxin (mToxin) on α7 nicotinic acetylcholine receptors (α7AChR). Using Creative Biogene's Ion Channel Screening & Profiling Services, PC12 cells expressing α7AChR were cultured and prepared for manual patch clamp recordings. Cells were seeded into 24-well plates with coverslips and incubated to reach appropriate confluency. The team applied mToxin and recorded receptor currents, generating quantitative data on its effects on α7AChR activity under controlled in vitro conditions.

Figure 2. Whole-cell patch-clamp recordings in PC12 cells showing that mToxin alone does not evoke currents but partially inhibits α7AChR-mediated responses induced by AR-R17779.Figure 2. Whole-cell patch-clamp recordings in PC12 cells showing that mToxin alone does not evoke currents but partially inhibits α7AChR-mediated responses induced by AR-R17779. (Fonar G, et al., 2021)

Contact Us

If you have any special requirements in ion channel compound screening, please feel free to contact us. We are looking forward to working together with your attractive projects.

References

  1. Bagal SK, Brown AD, Cox PJ, et al. Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624.
  2. Fonar G, Polis B, Sams DS, et al. Modified Snake α-Neurotoxin Averts β-Amyloid Binding to α7 Nicotinic Acetylcholine Receptor and Reverses Cognitive Deficits in Alzheimer's Disease Mice. Mol Neurobiol. 2021 May;58(5):2322-2341.
Publications
  1. Fonar G, Polis B, Sams D S, et al. Modified Snake α-Neurotoxin Averts β-Amyloid Binding to α7 Nicotinic Acetylcholine Receptor and Reverses Cognitive Deficits in Alzheimer’s Disease Mice[J]. Molecular neurobiology, 2021, 58: 2322-2341.
* For research use only. Not intended for any clinical use.
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