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Felodipine Europäischer Partner

ArtNr S1885-100
Hersteller Selleckchem
CAS-Nr. 72509-76-3
Menge 100 mg
Quantity options 10 mg 100 mg 10 mM/1 ml 200 mg 25 mg 50 mg
Kategorie
Typ Inhibitors
Specific against other
Smiles CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias CGH-869
Similar products Felodipine
Lieferbar
Manufacturer - Targets
CA2
Storage Conditions
2 years -80 in solvent
Molecular Weight
384, 25
Administration
Orally
Animal Models
Male Sprague-Dawley rats with approximately 5/6 renal ablation
Clinical Trials
A Phase I study to evaluate the pharmacokinetic interaction between Candesartan and Felodipine in a combination package compared to the separate intake of the reference brands Atacand and Splendil after a fasting period has been completed.
Dosages
1 g/kg/day
Formulation
Dissolved in DMSO, and diluted in saline
IC50
0.15 nM [1], 0.15 nM [1], 0.15 nM [1], 0.15 nM [1], 0.15 nM [1], 0.15 nM [1]
In vitro
Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ca.50 times more potent than nifedipine (IC50 of ca.8 nM) and ca.430 times than verapamil (IC50 of ca.65 nM). [1] Felodipine significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes. [2] Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM. [3] Felodipine at low concentration of 0.1 uM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells. [4] Felodipine (10 uM) reduces nuclear translocation of p42/44 mitogen-activated protein kinase and Elk-1 activation stimulated by PDGF-BB, leading to the inhibition of human SMC proliferation. [5] Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 uM. [6]
In vivo
Oral administration of Felodipine significantly reduces the average blood pressure (BP) in rats with 5/6 renal ablation, but causes additional impairment of the already impaired renal autoregulation. [7] Administration of Felodipine significantly reduces systolic blood pressure (SBP), serum insulin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by blocking NF-kappaB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. [8]
Kinase Assay
The effect of Felodipine on tension in coronary segments, The cylindrical coronary segments from porcine hearts are inverted and fixed horizontally between a stationary bottom pin and a top pin connected to the lever of a force-displacement transducer precalibrated with standard weights on a Grass model 5D polygraph. The cylindrical segments are bathed in 25 mL of PSS in a water jacketed tissue bath at 37 C. The bath solution is bubbled continuously with a mixture of 95% O2-5% CO2. An initial resting tension of 10 g is set during a 2-hour equilibration period. After the equilibration, three to four successive contraction-relaxation cycles are induced with 35 mM KCl and subsequent washes with PSS until reproducible contractions are obtained. After the final response reached and maintained steady tension (16-25 g above resting tension), a cumulative dose-response curve for Felodipine is obtained. Additional aliquots of Felodipine are added only after the response to the previous dose has plateaued. The concentration of Felodipine that half-maximally relaxes the coronary from KCl-induced contraction (IC50) is determined from dose response curve.
Solubility (25C)
DMSO 77 mg/mL, Water <1 mg/mL, Ethanol 72 mg/mL
Information
Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
Features
Unlike many other Ca2+ channel blockers, Felodipine does not exhibit cardiac side effects due to its significant selectivity toward vascular smooth muscle relative to myocardial tissue.

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 100 mg
Lieferbar: In stock
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