TRPV4 antagonist-7
TRPV4 antagonist-7 is a potent and selective TRPV4 antagonist with an IC50 of 0.2 nM against human targets. TRPV4 antagonist-7 binds to the voltage-sensor-like domain cavity of TRPV4 and inhibits channel activity through the formation of salt bridges, hydrogen bonds, and edge-to-face π-stacking interactions. TRPV4 antagonist-7 induces phospholipid accumulation in HepG2 C3A cells in vitro with an IC50 of 3.8 μM, and exhibits moderate inhibitory effects on CYP2D6 with an IC50 of 5.1 μM. TRPV4 antagonist-7 dose-dependently inhibits GSK1016790A (HY-19608)-induced bronchoconstriction in rats and cough in guinea pigs. TRPV4 antagonist-7 can be used in studies related to respiratory system diseases.
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: 3050594-88-9
- 分子式: C26H30ClFN4O3
- 分子量:500.99
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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
- 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 0.2 nM (IC50) |
CYP2D6 5.1 μM (IC50) |
体外実験
TRPV4 antagonist-7 (compound 39) (10 min) potently inhibits hTRPV4-mediated calcium mobilization in primary human airway smooth muscle cells, with an IC50 of 0.2 nM[1].
TRPV4 antagonist-7 (4 μM; 120 min) exhibits favorable metabolic stability in cryopreserved hepatocytes across species, with the highest intact fraction observed in canine hepatocytes (97.0%) and the lowest in miniature pig hepatocytes (77.1%)[1].
TRPV4 antagonist-7 exhibits moderate inhibitory activity against human CYP2D6 (IC50 = 5.1 μM), with a low risk of inhibiting other major human CYP subtypes[1].
TRPV4 antagonist-7 inhibits hERG channels with an IC50 of 2743 nM, indicating a controllable safety margin relative to its potency against hTRPV4[1].
TRPV4 antagonist-7 exhibits high intrinsic permeability in Caco-2 cells, with an efflux ratio of 31, which is significant yet controllable[1].
TRPV4 antagonist-7 exhibits favorable solubility (274 μM), moderate human liver microsomal stability (HLM Clint = 21 μL/min/mg), and a human plasma free fraction of 5%[1].
TRPV4 antagonist-7 (0.0099-10 μM; 24 h) induces phospholipidosis in human HepG2 clone C3A cells, with an IC50 of 3.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
TRPV4 antagonist-7 (0.03-10 mg/kg; p.o.; single administration) dose-dependently inhibits GSK1016790A-induced cough in Dunkin-Hartley guinea pigs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Brown Norway (male, 225-250 g)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited GSK1016790A-induced bronchoconstriction.
Significantly reduced PenH values compared to vehicle-treated challenged rats at doses of 0.3 mg/kg and above.
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Animal Model:Dunkin-Hartley (male, 300-500 g)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited GSK1016790A-induced cough.
Significantly reduced the number of coughs compared to vehicle-treated challenged guinea pigs at doses of 0.3 mg/kg, 1 mg/kg, 3 mg/kg, and 10 mg/kg.
化学情報
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CAS 番号 3050594-88-9
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分子量 500.99
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分子式 C26H30ClFN4O3
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SMILES
O=C(NC1=CC(Cl)=C(C=C1)CN2CCC[C@]([C@@](C)(CO)O)(C2)[H])C3=CN(N=C3C)C4=CC=C(C=C4)F
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TRPV4 antagonist-7 関連分類
HY-187364 関連分類
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