Name: Amlodipine besylate
Brand: Alomone Labs
SKU: A-120
Availability: InStock

Cat #: A-120

Alternative Name Norvasc^®

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 567.1

Purity: >99%

Effective concentration 1-100 μM.

Structure

Chemical name 2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester benzenesulfonate.

Molecular formula C₂₀H₂₅ClN₂O₅*C₆H₆O₃S.

CAS No.: 111470-99-6

Activity Amlodipine besylate is a dihydropyridine that acts as an L-type voltage-gated Ca²⁺ channel blocker and is used in the clinic to treat hypertension^1,2. Amlodipine besylate inhibits L- and T-type Ca_V channels with similar potency³.

References-Activity

Burges, R.A. et al. (1987) J. Cardiovasc. Pharmacol. 9, 110.
Julius, S. et al. (2004) Lancet 363, 2022.
Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol. 45, 241.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs Amlodipine besylate blocks L-type Ca²⁺ currents in Xenopus oocytes.
A. Time course of L-type channel (Ca_V1.2+α2δ1+β1a) activity before and during applications of 100 μM Amlodipine besylate (#A-120) (green) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. B. Example current traces before (black) and during application of 100 μM Amlodipine besylate (taken from the experiment described in A).

References - Scientific background

Hockerman, G.H. et al. (1997) Annu. Rev. Pharmacol. Toxicol. 37, 361.
Haller, H. (2008) Int. J. Clin. Pract. 62, 781.
Julius, S. et al. (2004) Lancet 363, 2022.
Burges, R.A. et al. (1987) J. Cardiovasc. Pharmacol. 9, 110.
Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol. 45, 241.

Scientific background

L-type (Ca_V1) voltage-gated Ca²⁺ channels are plasma membrane protein complexes which allow the passage of Ca²⁺ ions into cells following depolarization of the membrane potential. L-type channels are widely expressed in cardiac and smooth muscle where they control contraction. Consequently, these channels were recognized as a therapeutic target for cardiovascular diseases^1,2.

Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels. Many are used in the clinic to treat hypertension^2,3. Amlodipine besylate is a DHP that acts as an L-type, voltage-gated Ca²⁺ channel blocker and is used in the clinic to treat hypertension^3,4. Amlodipine inhibits Ca²⁺-induced contractions in depolarised rat aorta (IC₅₀ 1.9 nM) but displays a very slow action onset. Contractions induced by depolarising steps with 45 mM K⁺ are far less potently blocked by amlodipine (IC₅₀ 19.4 nM) and guinea pig papillary muscle single-cell slow action potentials are blocked at a concentration of 5 mM⁴. Amlodipine besylate inhibits L- and T-type Ca_V channels with similar potency⁵.

Target L-type and T-type Ca²⁺channels

Lyophilized Powder

Last update: 24/12/2020

Amlodipine besylate (#A-120) is a highly pure, synthetic, and biologically active compound.

Order Summary

Sign In

Amlodipine besylate

In wishlist

Applications

Specifications

Scientific Background

Citations

Related Products

Resources

Need Help With This Product?

Amlodipine besylate In wishlist