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Our Bioassay
- 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.
- Alomone Labs Amlodipine besylate blocks L-type Ca2+ currents in Xenopus oocytes.A. Time course of L-type channel (CaV1.2+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).
- 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.
L-type (CaV1) 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 diseases1,2.
Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels. Many are used in the clinic to treat hypertension2,3. Amlodipine besylate is a DHP that acts as an L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. 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 CaV channels with similar potency5.
Amlodipine besylate (#A-120) is a highly pure, synthetic, and biologically active compound.
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Specifications
Scientific Background
Citations
Related Products
Antibodies
- Anti-CaV1.1 (CACNA1S) (extracellular) Antibody (#ACC-314)
- Anti-CaV1.2 (CACNA1C) Antibody (#ACC-003)
- Guinea pig Anti-CaV1.2 (CACNA1C) Antibody (#AGP-001)
- Anti-Human CaV1.2 (CACNA1C) Antibody (#ACC-022)
- Anti-CaV1.3 (CACNA1D) Antibody (#ACC-005)
- Anti-CaV1.3 (CACNA1D) (extracellular) Antibody (#ACC-311)
- Anti-CACNA1G (CaV3.1) Antibody (#ACC-021)
- Anti-CACNA1G (CaV3.1)-ATTO Fluor-594 Antibody (#ACC-021-AR)
- Anti-CaV3.2 (CACNA1H) Antibody (#ACC-025)
- Anti-CaV3.3 (CACNA1I) Antibody (#ACC-009)
Pharmacological tools
Explorer kits & Research packs
- CaV1.2 (CACNA1C) Channel Basic Research Pack (#ESB-100)
- CaV1.2 (CACNA1C) Channel Premium Research Pack (#ESP-100)
- CaV1.2 (CACNA1C) Channel Deluxe Research Pack (#ESD-100)
- T-Type CaV Channel Basic Research Pack (#ESB-101)
- T-Type CaV Channel Premium Research Pack (#ESP-101)
- T-Type CaV Channel Deluxe Research Pack (#ESD-101)
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