Amlodipine besylate
Biological Activity
L-type calcium channel blocker that displays antihypertensive properties. Inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease. Inhibits proliferation of human vascular smooth muscle cells and epidermoid carcinoma A431 cells (IC50 = 25 μM).
Compound Libraries
Amlodipine besylate is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 567.05 |
| Formula | C20H25ClN2O5.C6H6O3S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 111470-99-6 |
| PubChem ID | 60496 |
| InChI Key | ZPBWCRDSRKPIDG-UHFFFAOYSA-N |
| Smiles | OS(=O)(=O)C1=CC=CC=C1.CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.67 | 10 | |
| DMSO | 56.7 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 567.05. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.76 mL | 8.82 mL | 17.64 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.53 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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References
References are publications that support the biological activity of the product.
Burges et al (1987) 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. 9 110 PMID: 2434785
Yoshida et al (2003) Antiproliferative effect of Ca2+ channel blockers on human epidermoid carcinoma A431 cells. Eur.J.Pharmacol. 472 23 PMID: 12860469
Toba et al (2005) Calcium channel blockades exhibit anti-inflammatory and antioxidative effects by augmentation of endothelial nitric oxide synthase and the inhibition of angiotensin converting enzyme in the NG-nitro-L-arginine methyl ester-induced hype Hypertens.Res. 28 689 PMID: 16392774
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Keywords: Amlodipine besylate, Amlodipine besylate supplier, Ca2+, channel, blockers, L-type, Calcium, CaV, Channels, L-Type, voltage-gated, voltage-dependent, Norvasc, Voltage-gated, 2571, Tocris Bioscience
2 Citations for Amlodipine besylate
Citations are publications that use Tocris products. Selected citations for Amlodipine besylate include:
Sharma et al (2016) Suppression of protective responses upon activation of L-type voltage gated calcium channel in macrophages during mycobacterium bovis BCG infection PLoS One 11 e0163845 PMID: 27723836
Zhong et al (2014) Serotonin 5-HT3 receptor-mediated vomiting occurs via the activation of Ca2+/CaMKII-dependent ERK1/2 signaling in the least shrew (Cryptotis parva). PLoS One 9 e104718 PMID: 25121483
Do you know of a great paper that uses Amlodipine besylate from Tocris? Please let us know.
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L-type Ca2+ current was analysed by patch clamp in guinea pig ventricular cardiomyocytes before and after amlodipine (10 µM) superfusion. Amlodipine blocked calcium current density.
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