GSK3395879
GSK3395879 is a TRPV4 antagonist that acts on hTRPV4 with an IC50 of 1 nM. GSK3395879 blocks agonist-induced TRPV4-mediated Ca2+ mobilization. GSK3395879 inhibits rat pulmonary edema induced by the TRPV4 agonist GSK1016790A (HY-19608). GSK3395879 can be used in research related to heart failure.
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- CAS. Nr.: 2215852-91-6
- Formel: C20H15F4N3O5S
- Molecular Weight:485.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hTRPV4 1 nM (IC50) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (Male)[1]
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Dosage:0.03, 0.08, and 0.23 mg/kg (i.v. bolus loading dose); 0.6, 1.7, and 5.1 μg/kg/min (continuous i.v. infusion)
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Administration:i.v. bolus followed by continuous i.v. infusion; 60 min
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Result:Inhibited the GSK1016790A-induced decrease in MAP and increase in LW/BW ratio in a dose-dependent manner.
Achieved full inhibition of the GSK1016790A-induced decrease in MAP and increase in LW/BW at an infusion dose of 5.1 μg/kg/min.
Chemical Information
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CAS. Nr. 2215852-91-6
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Molecular Weight 485.41
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Formel C20H15F4N3O5S
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SMILES
FC1=C(C#N)C=CC(O[C@@H]2[C@@](CO)(O)CN(S(C3=C(C#N)C=C(C(F)(F)F)C=C3)(=O)=O)C2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Brnardic EJ, et al. Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). Journal of medicinal chemistry. 2018 Nov 08;61(21):9738-9755. [Content Brief]
[2]. Nilsson M, et al. TRPV4: A Promising Therapeutic Target Ion Channel─Discovery of Ultrapotent Selective Antagonists. Journal of medicinal chemistry. 2026 Jul 23;69(14):16926-16948. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GSK3395879 Related Classifications
HY-112202 Related Classifications
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