Amlodipine Inhibitor CAS No. 88150-42-9

Cat. No.	Name	Size	Price	Add Cart
KI0672	Amlodipine	50 mg	$155.2

Chemical Characteristic

Product Name	Amlodipine
Synonyms	Norvasc
CAS No.	88150-42-9
Molecular Weight	408.9
Formula	C₂₀H₂₅ClN₂O₅
Chemical Structure

Biological activities

Amlodipine is a long-acting calcium channel blocker. The IC50 of amlodipine is 1.9 nM against calcium channel. Amlodipine inhibits contractions induced by depolarising steps with 45 mM K⁺ with an IC50 of 19.4 nM.^[1]Amlodipine inhibits A431 cell growth and the incorporation of BrdU into cells in vitro. In the fluorimetric measurement of intracellular free Ca²⁺ concentration in fura-2 or fluo-3 loaded A431 cells, amlodipine blunts the thapsigargin- or cyclopiazonic acid-induced Ca²⁺ release from endoplasmic reticulum and the ensuing Ca²⁺ influx through Ca²⁺-permeable channels.^[2] Amlodipine potently reverses the resistance of topotecan in MDR HL-60 cells. Moreover, amlodipine enhances the apoptosis-inducing effect of topotecan synergistically in K562 and HL-60 cells.^[3] Amlodipine treatment (10 mg/kg/day orally) significantly reduces the increase in blood pressure (BP) in spontaneously hypertensive rats (SHR), but does not change BP in Wistar-Kyoto rats (WKY).^[4] Furthermore, amlodipine releases nitric oxide from canine coronary microvessels which are isolated from the heart of normal dogs.^[5]

Protocols

In vivo: Amlodipine is dissolved in 0.01% DMSO and PBS.^[5]

References

[1] Burges RA, et al. Calcium channel blocking properties of amlodipine in vascular smooth muscle and cardiac muscle in vitro: evidence for voltage modulation of vascular dihydropyridine receptors. J Cardiovasc Pharmacol. 1987, 9(1): 110-119. 閵嗏偓閵嗏偓 [2] Yoshida J, et al. Antiproliferative effect of Ca²⁺ channel blockers on human epidermoid carcinoma A431 cells. Eur J Pharmacol. 2003, 472(1-2): 23-31. [3] Li X, et al. Effect of stealthy liposomal topotecan plus amlodipine on the multidrug-resistant leukaemia cells in vitro and xenograft in mice. Eur J Clin Invest. 2006, 36(6): 409-418. [4] Morel N, et al. Selective interaction of the calcium antagonist amlodipine with calcium channels in arteries of spontaneously hypertensive rats. J Cardiovasc Pharmacol. 1994, 24(4): 524-533. 閵嗏偓閵嗏偓 [5] Zhang X, et al. Amlodipine releases nitric oxide from canine coronary microvessels: an unexpected mechanism of action of a calcium channel-blocking agent. Circulation. 1998, 97(6): 576-580. 閵嗏偓閵嗏偓

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