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Cat. No.: HY-182455

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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.

CAS No.: 2215855-22-2
Formula: C₁₇H₁₆ClFN₄O₄S
Molecular Weight:426.85

Storage:

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

GSK3527497 Chemical Structure

CAS No.: 2215855-22-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target^[1]

TRPV4

All TRP Channel Isoforms :

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.

Parmacokinetics

Species	Dose	Route	MRT	CL	V_dss	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 %

Chemical Information

CAS No. 2215855-22-2
Molecular Weight 426.85
Formula C₁₇H₁₆ClFN₄O₄S
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

Handling Instructions (2659 KB)

References

[1]. Brooks CA, et al. Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem. 2019;62(20):9270-9280. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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