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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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 2215855-22-2
Formule: C₁₇H₁₆ClFN₄O₄S
Masse moléculaire:426.85

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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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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
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Activité biologique

Description

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

IC₅₀ & Target^[1]

TRPV4

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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
Masse moléculaire 426.85
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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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.

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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GSK3527497

Voir tous les produits spécifiques à Isoform TRP Channel

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

GSK3527497 Related Classifications

HY-182455 Related Classifications