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Felodipine

Catalog No. T0145 CAS 72509-76-3

Synonyms: CGH-869

Felodipine (CGH-869) is a longlasting 1, 4-dihydropyridine calcium channel repressor.

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Felodipine, CAS 72509-76-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 75.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 189.00
100 mg	In stock	$ 278.00
200 mg	In stock	$ 418.00
500 mg	In stock	$ 682.00
1 mL * 10 mM (in DMSO)	In stock	$ 83.00

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Purity: 98.31%

Biological Description

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Storage & Solubility Information

Description	Felodipine (CGH-869) is a longlasting 1, 4-dihydropyridine calcium channel repressor.
Targets&IC50	Ca2+ channel, L-type:0.15 nM
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.

Synonyms	CGH-869
Molecular Weight	384.25
Formula	C18H19Cl2NO4
CAS No.	72509-76-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 38.4 mg/mL (100 mM)

Ethanol: 38.4 mg/mL (100 mM)

References and Literature

1. Johnson JD, et al. J Pharmacol Exp Ther, 1983, 226(2), 330-334. 2. Rödler S, et al. J Mol Cell Cardiol, 1995, 27(10), 2295-2302. 3. Yiu S, et al. J Med Chem, 1996, 39(23), 4576-4582. 4. Ding Y, et al. Hypertension, 1998, 32(4), 718-723. 5. Yang Z, et al. Cardiovasc Res, 2002, 53(1), 227-231.

Citations

1. Wang B, Pei J, Zhang H, et al.Dihydropyridine-derived calcium channel blocker as a promising anti-hantavirus entry inhibitor.Interventions for emerging infectious diseases.2023, 16648714.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Anti-Hypertension Compound Library Neuronal Signaling Compound Library Anti-Metabolism Disease Compound Library Anti-Cancer Compound Library

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Keywords

Felodipine 72509-76-3 Autophagy Membrane transporter/Ion channel Metabolism Calcium Channel Inhibitor dihydropyridine smooth CGH 869 vascular inhibit CGH869 blood Ca2+ channels muscle pressure Ca channels L-type CGH-869 inhibitor

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