Monatepil
Monatepil (AJ-2615 free base) is a calcium antagonist with potent α1-adrenoceptor blocking activity. Monatepil inhibits vasopressin- or methacholine-induced ischemic electrocardiographic changes in a rat model of vasospastic angina and reduces the mean arterial pressure in anesthetized rats. Monatepil also enhances low-density lipoprotein (LDL) receptor activity in human skin fibroblasts. Monatepil can be used in research related to hypertension, atherosclerosis, hyperlipidemia and vasospastic angina.
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: 103377-41-9
- 分子式: C28H30FN3OS
- 分子量:475.63
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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
[2]|
α1-adrenergic receptor |
Calcium Channel |
体外実験
Monatepil (AJ-2615 free base) enhances LDL receptor activity in human skin fibroblasts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Monatepil (0.3 mg/kg; i.v.) significantly inhibits acetylcholine (16 μg/kg; intracoronary administration)-induced ST-segment elevation in male Jcl:Sprague-Dawley rats; the inhibition rate exceeds 60% at a dose of 1 mg/kg[2].
Monatepil (0.1-1 mg/kg; i.v.) reduces the mean arterial pressure of anesthetized male Std:Wistar rats by 14.0, 40.6, and 50.2 mmHg, respectively; at doses of 0.3 and 1 mg/kg, it also significantly decreases heart rate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Nrc:Donryu rats, 120-190 g; vasopressin (0.2 IU/kg, i.v.)-induced ischemic ST-segment depression[2]
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Dosage:3 mg/kg; 30 mg/kg
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Administration:Oral administration (p.o.)
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Result:Significantly inhibited vasopressin-induced ST-segment depression at 3 mg/kg; significant inhibition remained 7 h after 30 mg/kg.
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Animal Model:Male Jcl:Sprague-Dawley rats, ~500 g; methacholine (16 μg/kg, intracoronary arterial administration)-induced ST-segment elevation[2]
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Dosage:0.3 mg/kg; 1 mg/kg
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Administration:Intravenous administration (i.v.)
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Result:Significantly inhibited ST-segment elevation at 0.3 mg/kg and produced >60% inhibition at 1 mg/kg.
化学情報
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CAS 番号 103377-41-9
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分子量 475.63
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分子式 C28H30FN3OS
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SMILES
O=C(NC1C=2C=CC=CC2SCC=3C=CC=CC31)CCCN4CCN(C5=CC=C(F)C=C5)CC4
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別名
AJ-2615 free base
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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)
Monatepil 関連分類
HY-106818 関連分類
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