GSK3395879

Modify Date: 2025-12-27 08:26:49

GSK3395879 Structure
GSK3395879 structure
Common Name GSK3395879
CAS Number 2215852-91-6 Molecular Weight 485.41
Density N/A Boiling Point N/A
Molecular Formula C20H15F4N3O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK3395879


GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4[1].

 Names

Name GSK3395879

 GSK3395879 Biological Activity

Description GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4[1].
Related Catalog
Target

IC50: 1 nM (hTRPV4)[1]

References

[1]. Brnardic EJ, et al. Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem. 2018 Nov 8;61(21):9738-9755.

 Chemical & Physical Properties

Molecular Formula C20H15F4N3O5S
Molecular Weight 485.41
InChIKey RAYCYIKGBWRQBC-RBUKOAKNSA-N
SMILES N#Cc1ccc(OC2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3C#N)CC2(O)CO)cc1F

 GSK3395879Bioassay

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Name: Ratio of Cmax to Cmin in human
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322961
Name: Drug metabolism in rat hepatocytes assessed as oxidation of arene oxide metabolite by...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322958
Name: Drug metabolism in rat hepatocytes assessed as rearomatization/conjugation by measuri...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322957
Name: Drug metabolism in rat hepatocytes assessed as GSH-mediated sulfonamide cleavage by m...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322956
Name: Ratio of unbound clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as 30 mi...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322955
Name: In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib...
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL4158460
Name: In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib...
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL4158461
Name: In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib...
Source: ChEMBL
Target: Rattus norvegicus
External Id: CHEMBL4158462
Name: Oral bioavailability in Sprague-Dawley rat at 1 mg/kg by HPLC-MS/MS analysis
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322943
Name: Dose normalized AUC in Sprague-Dawley rat at 1 mg/kg, po by HPLC-MS/MS analysis
Source: ChEMBL
Target: N/A
External Id: CHEMBL4322942
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