Monatepil maleate
Monatepil (AJ-2615 free base) maleate is a calcium antagonist with potent α1-adrenoceptor blocking activity. Monatepil maleate 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 maleate also enhances low-density lipoprotein (LDL) receptor activity in human skin fibroblasts. Monatepil maleate can be used in research related to hypertension, atherosclerosis, hyperlipidemia and vasospastic angina.
For research use only. We do not sell to patients.
- CAS No.: 103379-03-9
- Formula: C32H34FN3O5S
- Molecular Weight:591.69
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
α1-adrenergic receptor |
Calcium Channel |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Monatepil maleate (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 maleate (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.
Chemical Information
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CAS No. 103379-03-9
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Molecular Weight 591.69
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Formula C32H34FN3O5S
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SMILES
OC(/C=C\C(O)=O)=O.FC(C=C1)=CC=C1N(CC2)CCN2CCCC(NC3C4=CC=CC=C4CSC5=CC=CC=C53)=O
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Synonyms
AJ-2615
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Monatepil maleate Related Classifications
HY-106818A Related Classifications
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