1. Membrane Transporter/Ion Channel
  2. TRP Channel

TRPC6-IN-1 

Cat. No.: HY-101547
Handling Instructions

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

For research use only. We do not sell to patients.

TRPC6-IN-1 Chemical Structure

TRPC6-IN-1 Chemical Structure

CAS No. : 901715-05-7

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5099 mL 12.5493 mL 25.0985 mL
5 mM 0.5020 mL 2.5099 mL 5.0197 mL
10 mM 0.2510 mL 1.2549 mL 2.5099 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

398.43

Formula

C₂₁H₂₃FN₄O₃

CAS No.

901715-05-7

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TRPC6-IN-1
Cat. No.:
HY-101547
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TRPC6-IN-1

Cat. No.: HY-101547