product name Felodipine
Description: Felodipine (also known as CGH-869) is a selective L-type Ca2+ channel blocker of the 1,4-dihydropyridine class with IC50 of 0.15 NM. Felodipine is described to inhibit cytokine-induced NO and superoxide production as well as cytokine-induced NO synthase (NOS) mRNA induction, and is suggested to act as a scavenger of superoxide and not an inhibitor of inducible NOS induction. This indicates that Felodipine further protects the vasculature against endogenous free radical generation during inflammatory responses.
References: J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302.
384.25
Formula
C18H19Cl2NO4
CAS No.
72509-76-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 77 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 77 mg/mL (200.4 mM)
Solubility (In vivo)
Synonyms
CGH-869
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403632
| In Vitro |
In vitro activity: Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM). 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. 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. Felodipine at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells. Felodipine (10 μM) 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. Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302. |
Related Posts
product name Felodipine
Description: Felodipine (also known as CGH-869) is a selective L-type Ca2+ channel blocker of the 1,4-dihydropyridine class with IC50 of 0.15 NM. Felodipine is described to inhibit cytokine-induced NO and superoxide production as well as cytokine-induced NO synthase (NOS) mRNA induction, and is suggested to act as a scavenger of superoxide and not an inhibitor of inducible NOS induction. This indicates that Felodipine further protects the vasculature against endogenous free radical generation during inflammatory responses.
References: J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302.
384.25
Formula
C18H19Cl2NO4
CAS No.
72509-76-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 77 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 77 mg/mL (200.4 mM)
Solubility (In vivo)
Synonyms
CGH-869
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403632
| In Vitro |
In vitro activity: Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM). 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. 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. Felodipine at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells. Felodipine (10 μM) 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. Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302. |