[CAS NO. 72509-76-3] Felodipine
PRODUCTS SPECIFICATIONS [72509-76-3]
DESCRIPTION [72509-76-3]
Overview
| MDL | MFCD00868316 |
|---|---|
| Molecular Weight | 384.25 |
| Molecular Formula | C18H19Cl2NO4 |
| SMILES | O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OCC |
1 Publications Citing Use of MCE
Summary
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy . Felodipine can cross the blood-brain barrier [1] [2] [3] .
In Vitro
Felodipine, a dihydropyridine calcium antagonist, is the most potent in relaxing porcine coronary arteries (IC
50
=0.15 nM)
[1]
.
Felodipine, an L-type calcium channel blocker, induces autophagy and clears diverse aggregate-prone, neurodegenerative disease-associated proteins
[2]
.
Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC
50
of 1.45 nM
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05614037 | Overseas Pharmaceuticals, Ltd.|Guangzhou Kangqi Medical Technology Co., LTD |
Hypertension
|
October 28, 2022 | Phase 1 |
| NCT00348686 | AstraZeneca |
Hypertension|Left Ventricular Hypertrophy
|
June 2006 | Phase 4 |
| NCT01238705 | LanZhou University |
Hypertension|Sexual Dysfunction
|
April 2008 | Phase 4 |
| NCT01630902 | Torrent Pharmaceuticals Limited |
Healthy
|
Phase 1 | |
| NCT00861016 | AstraZeneca |
Hypertension
|
October 2005 | Phase 4 |
| NCT00742066 | Maastricht University Medical Center |
Hypertension|Insulin Resistance|Microcirculation
|
March 2008 | Not Applicable |
| NCT02336607 | AstraZeneca |
Hypertension
|
December 2005 | Not Applicable |
| NCT02744872 | Rigshospitalet, Denmark |
Disorder Related to Lung Transplantation
|
September 2013 | Phase 4 |
| NCT00905333 | AstraZeneca|Scentryphar Clinical Research|Cori Analyticals|Clínica São Lucas, Hospital Sírio Libanês de Itatiba S+C|LabClin Laboratório Clínico|Laboratório de Patologia Clínica Dr. Franceschi Ltda.|Faculty of Pharmaceutical Sciences of Ribeirão Preto - Bioequivalence Center |
Healthy
|
October 2008 | Phase 1 |
| NCT01136863 | Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Shanxi Kangbao Pharmaceutical company|Beijing Hypertension League Insititute |
Hypertension
|
April 1998 | Not Applicable |
| NCT01630655 | Torrent Pharmaceuticals Limited |
Healthy
|
Phase 1 | |
| NCT02327247 | Ranbaxy Laboratories Limited|Ranbaxy Inc. |
Healthy
|
September 2008 | Not Applicable |
| NCT01520285 | Lee´s Pharmaceutical Limited |
Hypertension
|
December 2011 | Phase 4 |
| NCT02232269 | Lawson Health Research Institute |
Food-Drug Interactions
|
February 2012 | Phase 1 |
| NCT02311530 | Ranbaxy Laboratories Limited|Ranbaxy Inc. |
Healthy
|
October 2008 | Not Applicable |
| NCT00841880 | Sanofi |
Hypertension
|
January 2009 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 260.25 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6025 mL | 13.0124 mL | 26.0247 mL |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2049 mL |
| 10 mM | 0.2602 mL | 1.3012 mL | 2.6025 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
References
- [1] Johnson JD, et al. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330-334.
- [2] Siddiqi FH, et al. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing [published correction appears in Nat Commun. 2019 Jun 4;10(1):2530]. Nat Commun. 2019;10(1):1817. Published 2019 Apr 18.
- [3] Yiu, S. and E.E. Knaus, Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem, 1996. 39(23): p. 4576-82.
Synonyms