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Cat. No.: 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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CAS No.: 103377-41-9
화학식: C₂₈H₃₀FN₃OS
분자량:475.63

보관:

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

Monatepil Chemical Structure

CAS No.: 103377-41-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[2]

α1-adrenergic receptor

Calcium Channel

All Adrenergic Receptor Isoforms :

All Calcium Channel Isoforms :

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

CAS No. 103377-41-9
분자량 475.63
화학식 C₂₈H₃₀FN₃OS
SMILES

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

AJ-2615 free base
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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.

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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Help & FAQs

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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Monatepil

All Adrenergic Receptor Isoforms

All Calcium Channel Isoforms