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Referencia número: HY-106818

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Monatepil

Name: Monatepil
Brand: MedChemExpress
SKU: HY-106818
Availability: PreOrder

(Synonyms: AJ-2615 free base)

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.

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No. CAS: 103377-41-9
Fòrmula: C₂₈H₃₀FN₃OS
Peso molecular:475.63

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Monatepil Chemical Structure

No. CAS: 103377-41-9

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Actividad biológica

Descripciòn

IC₅₀ & Target

^[2]

α1-adrenergic receptor

Calcium Channel

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In Vitro

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.

In Vivo

Monatepil (AJ-2615 free base) (3 mg/kg; p.o.; 1 h prior to vasopressin administration) significantly inhibits vasopressin (0.2 IU/kg; i.v.)-induced ST-segment depression in male Nrc:Donryu rats; a significant inhibitory effect remains 7 h after oral administration of 30 mg/kg^[2].
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.

Animal Model:

Male Nrc:Donryu rats, 120-190 g; vasopressin (0.2 IU/kg, i.v.)-induced ischemic ST-segment depression^[2]
Dosage:

3 mg/kg; 30 mg/kg
Administration:

Oral administration (p.o.)
Result:

Significantly inhibited vasopressin-induced ST-segment depression at 3 mg/kg; significant inhibition remained 7 h after 30 mg/kg.

Animal Model:

Male Jcl:Sprague-Dawley rats, ~500 g; methacholine (16 μg/kg, intracoronary arterial administration)-induced ST-segment elevation^[2]
Dosage:

0.3 mg/kg; 1 mg/kg
Administration:

Intravenous administration (i.v.)
Result:

Significantly inhibited ST-segment elevation at 0.3 mg/kg and produced >60% inhibition at 1 mg/kg.

Chemical Information

No. CAS 103377-41-9
Peso molecular 475.63
Fòrmula C₂₈H₃₀FN₃OS
SMILES

O=C(NC1C=2C=CC=CC2SCC=3C=CC=CC31)CCCN4CCN(C5=CC=C(F)C=C5)CC4
Synonyms

AJ-2615 free base
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Miyazaki M, et al. Antihypertensive, antiatherosclerotic, and plasma lipid-lowering effects of monatepil, a novel calcium antagonist with alpha 1-adrenoceptor-blocking activity in experimental animals. American journal of hypertension. 1994 Oct;7(10 Pt 2):131S-40S.

[2]. Yamamoto T, et al. Preventive effect of a new calcium antagonist, monatepil, on drug-induced ischaemic electrocardiographic changes in rats. Clinical and experimental pharmacology & physiology. 1993 Nov;20(11):673-8.

[3]. Sasaki J, et al. Comparative effects of monatepil, a novel calcium antagonist with alpha 1-adrenergic-blocking activity, and nitrendipine on lipoprotein and carbohydrate metabolism in patients with hypertension. American journal of hypertension. 1994 Oct;7(10 Pt 2):161S-166S.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Monatepil

Ver todos los productos específicos de isoformas Adrenergic Receptor

Ver todos los productos específicos de isoformas Calcium Channel