Amlodipine mesylate

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Amlodipine mesylate 

Amlodipine mesylate 是一种抗心绞痛药和具有口服活性二氢吡啶钙通道（calcium channel）阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine mesylate 可用于高血压和癌症的研究。

Amlodipine mesylate

Amlodipine mesylate Chemical Structure

CAS No. : 246852-12-0

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Amlodipine mesylate 的其他形式现货产品:

Amlodipine Amlodipine maleate Amlodipine besylate

生物活性

Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target

L-type calcium channel

 

体外研究
(In Vitro)

Amlodipine mesylate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine mesylate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine mesylate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Amlodipine mesylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine mesylate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.

分子量

504.98

Formula

C21H29ClN2O8S
CAS 号

246852-12-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Kishen G. Bulsara, et al. Amlodipine.

    [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

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