P552-02
P552-02 is an epithelial sodium channel (ENaC) inhibitor. P552-02 blocks ENaC function in humans, guinea pigs, rats and sheep, exhibits the characteristic of reduced dissociation rate after binding to ENaC, inhibits ENaC-mediated short-circuit current, and slows the absorption of airway surface liquid (ASL). P552-02 induces hyperkalemia in guinea pigs and rats, blocks the activity of airway ENaC in guinea pigs, and enhances mucociliary clearance in sheep both in vivo and in vitro. P552-02 is applicable to cystic fibrosis-related research.
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: 587879-32-1
- 分子式: C19H26ClN7O4
- 分子量:451.91
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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
P552-02 potently inhibits ENaC-mediated short-circuit current in primary human bronchial cells (pIC50 = 8.62), guinea pig ENaC (pIC50 = 8.42), and rat ENaC (pIC50 = 8.46), and exerts strong inhibitory activity against wild-type human ENaC in transfected FRT cells with a pIC50 of 8.85; mutations at the amiloride binding site drastically reduce its potency, with 4316-fold and 435-fold pIC50 shifts for αβG525Aγ and αβγG537C respectively[1].
P552-02 (250 nM; 2-10 min) exerts a moderately long-lasting blocking effect on ENaC in primary human bronchial epithelial cells, with 73.7% recovery of ISC after 2 min of incubation at 250 nM and 82.9% recovery after 10 min of incubation[1].
P552-02 potently inhibits ENaC-mediated short-circuit current in cultured human bronchial epithelial cells; it blocks the sustained absorption of airway surface liquid (ASL) in vitro, and acts synergistically with hypertonic saline to maintain the hydration state of ASL without blocking aquaporins[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | T1/2 |
|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 149 mL/min/kg | 19.7 L/kg | 3.8 h |
P552-02 (200-2000 μg/kg; intratracheal administration; single dose) induces dose-dependent hyperkalemia in rats following intratracheal administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin Hartley (male, 300-650 g)[1]
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Dosage:0.2 μg/kg (TPD assessment at 1 h); 128 μg/kg (TPD assessment at 4 h)
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Administration:i.t.; single dose
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Result:Attenuated tracheal potential difference with an ED50 of 0.2 μg/kg at 1 h after dosing.
Retained airway ENaC-blocking activity with an ED50 of 128 μg/kg at 4 h after dosing.
Induced a significant elevation in blood potassium levels relative to vehicle control at doses ≥ 60 μg/kg.
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Animal Model:Sprague-Dawley (male, 250-350 g)[1]
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Dosage:200, 600, 2000 μg/kg
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Administration:i.t.; single dose
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Result:Induced significant increases in blood potassium levels relative to vehicle control at 600 μg/kg (mean maximum level 6.53 mmol/L) and 2000 μg/kg (mean maximum level 6.95 mmol/L).
化学情報
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CAS 番号 587879-32-1
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分子量 451.91
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分子式 C19H26ClN7O4
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SMILES
O=C(NC(=N)NCCCCC1=CC=C(OCC(O)CO)C=C1)C2=NC(Cl)=C(N=C2N)N
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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)
P552-02 関連分類
HY-187082 関連分類
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