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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2215852-91-6
- 分子式: C20H15F4N3O5S
- 分子量:485.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
hTRPV4 1 nM (IC50) |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
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.
化学情報
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CAS 番号 2215852-91-6
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分子量 485.41
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GSK3395879 関連分類
HY-112202 関連分類
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