2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. GSK3527497

GSK3527497 is an orally active TRPV4 inhibitor. GSK3527497 is applicable for the research of heart failure.

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

GSK3527497

GSK3527497 Chemical Structure

CAS No. : 2215855-22-2

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GSK3527497 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

View All Isoforms
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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Description

GSK3527497 is an orally active TRPV4 inhibitor. GSK3527497 is applicable for the research of heart failure[1].

IC50 & Target[1]

TRPV4

 

In Vitro

GSK3527497 potently inhibits hTRPV4 with an IC50 of 12 nM in a FLIPR assay[1].
GSK3527497 inhibits hERG with an IC50 of 20 μM[1].
GSK3527497 inhibits CYP3A4 with an IC50 of 12 μM[1].

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

GSK3527497 Related Antibodies
Parmacokinetics
Species Dose Route MRT CL Vdss F
Rat[1] 1 mg/kg i.v. 2.5 h 45 mL/min/kg 6.7 L/kg /
Rat[1] 2 mg/kg p.o. / / / 26 %
Rat[1] 100 mg/kg p.o. / / / 87 %
Molecular Weight

426.85

Formula

C17H16ClFN4O4S
CAS No.
SMILES

NC[C@](O)(CN(C1)S(=O)(C2=CC=C(C=N2)Cl)=O)[C@H]1OC3=CC(F)=C(C=C3)C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSK3527497 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:

GSK35274972215855-22-2GSK 3527497GSK-3527497TRP ChannelTransient receptor potential channelshERGhTRPV4Sprague-Dawley ratsheart failureCYP3A4dogsTRPV4Inhibitorinhibitorinhibit

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