2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPC6-IN-1

TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.

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TRPC6-IN-1 Chemical Structure

TRPC6-IN-1 Chemical Structure

CAS No. : 901715-05-7

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Based on 1 publication(s) in Google Scholar

TRPC6-IN-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TRPC6-IN-1

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Description

TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.

IC50 & Target

EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3)[1].
Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.45 μM
Compound: 4o
Agonist activity at human TRPC3 expressed in HEK293 cells assessed as induction of membrane depolarization measured for 2.5 mins in presence of 0.5 mM Ca2+ by FLIPR membrane potential dye-based fluorescence assay
Agonist activity at human TRPC3 expressed in HEK293 cells assessed as induction of membrane depolarization measured for 2.5 mins in presence of 0.5 mM Ca2+ by FLIPR membrane potential dye-based fluorescence assay
[PMID: 28395140]
HEK293 EC50
0.497 μM
Compound: 4o
Agonist activity at human TRPC7 expressed in HEK293 cells assessed as increase in intracellular calcium level measured for 2.5 mins in presence of 2 mM Ca2+ by Fluo8-AM dye-based fluorescence assay
Agonist activity at human TRPC7 expressed in HEK293 cells assessed as increase in intracellular calcium level measured for 2.5 mins in presence of 2 mM Ca2+ by Fluo8-AM dye-based fluorescence assay
[PMID: 28395140]
HEK293 EC50
1.13 μM
Compound: 4o
Agonist activity at human TRPC7 receptor expressed in HEK293 cells assessed as induction of channel current in presence of 0.1 mM Ca2+ by whole cell patch-clamp method
Agonist activity at human TRPC7 receptor expressed in HEK293 cells assessed as induction of channel current in presence of 0.1 mM Ca2+ by whole cell patch-clamp method
[PMID: 28395140]
HEK293 EC50
4.7 μM
Compound: 62
Agonist activity at mouse TRPC4 expressed in HEK293 cells coexpressing M5 receptor assessed as induction of TRPC4-mediated calcium influx by fluorescence method
Agonist activity at mouse TRPC4 expressed in HEK293 cells coexpressing M5 receptor assessed as induction of TRPC4-mediated calcium influx by fluorescence method
[PMID: 30943030]
In Vitro

TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC50 value of 4.66±0.03 μM, demonstrating a comparable activity of the compound on TRPC6 as the original lead. TRPC6-IN-1 is also tested on HEK293 cells that co-expressed μ opioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by a μ agonist, these cells show a robust increase in [Ca2+]i. TRPC6-IN-1 also evokes whole-cell currents in HEK293 cells that express human TRPC3. TRPC6-IN-1 elicits concentration dependent current increases in the TRPC7 cells. Different from TRPC6, the currents show some desensitization in the high TRPC6-IN-1 concentrations (10 and 30 μM) at both negative and positive potentials even though the low Ca2+ (0.1 mM) bath solution is used. Nonetheless, a stepwise increase in the TRPC7 currents is still detected at <10 μM TRPC6-IN-1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TRPC6-IN-1 Related Antibodies
Molecular Weight

398.43

Formula

C21H23FN4O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC(C2=NC3=C(C4=CC=C(F)C=C4)C(C)=NN3C(O)=C2)CC1)OCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Purity & Documentation
References
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TRPC6-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRPC6-IN-1901715-05-7TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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