| Name | Felodipine |
| Description | Felodipine (CGH-869) is a longlasting 1, 4-dihydropyridine calcium channel repressor. |
| In vitro | Felodipine acts on the aortic wall by inhibiting NF-κB activation and effectively reduces serum insulin levels within macrophages, as well as intracellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1), thereby significantly lowering systolic blood pressure and modulating vascular inflammatory responses. Oral administration of Felodipine in rats with 5/6 nephrectomy markedly decreases the mean arterial blood pressure. |
| In vivo | In primary human VSMCs and lung fibroblasts, Felodipine significantly induced transcription and secretion of IL-6 (ED50: 5.8 nM) and IL-8 (ED50: 5.3 nM), with no effect observed from the administration of either propranolol or fenbufen on the expression of these IL genes. In guinea pig ileum longitudinal smooth muscle, Felodipine inhibited carbachol-regulated Ca2+-dependent contraction (IC50: 1.45 nM). At a concentration of 0.1 μM in rat endothelial cells, Felodipine increased NOx production and the activity of Ca2+-dependent NOS and eNOS proteins. At 10 μM, it suppressed human SMC proliferation by inhibiting PDGF-BB-induced Elk-1 activation and reducing the nuclear translocation of p42/44 mitogen-activated protein kinase. Felodipine moderately inhibited Cav3.2 T-type Ca2+ channels (IC50: 6.8 μM). In porcine coronary artery segments contracted with KCl, Felodipine significantly induced relaxation (IC50: 0.15 nM), suggesting it is 50 times more potent than nifedipine (IC50: ~8 nM) and 430 times more potent than verapamil (IC50: ~65 nM) due to its Ca2+ channel blocking action. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (650.62 mM), Sonication is recommended.
Ethanol : 38.4 mg/mL (99.93 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.2 mM), Sonication is recommended.
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| Keywords | vascular | smooth | pressure | muscle | L-type calcium channel | L-type | Inhibitor | inhibit | Felodipine | dihydropyridine | CGH869 | CGH 869 | CalciumChannel | Calcium Channel | Ca2+ channels | Ca channels | blood | Autophagy |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | 2,4,6-Tri-tert-butylphenol | Tamoxifen | Cysteamine hydrochloride | Guanidine hydrochloride | Hydroxychloroquine | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
