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Purity: ≥98%
Felodipine (formerly also known as CGH-869; trade names Plendil, Renedil etc.), a marketed anti-hypertensive drug, is a potent, selective and long-acting L-type Ca2+ channel blocker (CCB) of the 1,4-dihydropyridine (DHP) class with an IC50 of 0.15 nM. It was approved to treat high blood pressure in 1988. 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.
| ln Vitro |
The most efficient medication for relaxing pig coronary arteries is felodipine, a dihydropyridine calcium antagonist (IC50=0.15 nM) [1]. The L-type calcium channel blocker felodipine promotes autophagy and gets rid of a number of proteins linked to neurological diseases that are prone to aggregation [2]. With an IC50 of 1.45 nM, felodipine inhibits the contraction of guinea pig ileal longitudinal smooth muscle (GPILSM) mediated by muscarinic receptors (carbachol) in a Ca2+-dependent manner [3].
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| ln Vivo |
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| 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. |
| Molecular Formula |
C18H19CL2NO4
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| Molecular Weight |
384.25
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| CAS # |
72509-76-3
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| Related CAS # |
Felodipine-d3;1219795-30-8;Felodipine-d5;1242281-38-4
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| SMILES |
ClC1C(=C([H])C([H])=C([H])C=1C1([H])C(C(=O)OC([H])([H])[H])=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C1C(=O)OC([H])([H])C([H])([H])[H])Cl
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| InChi Key |
RZTAMFZIAATZDJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3
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| Chemical Name |
(RS)-3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05614037 | Active, not recruiting | Drug: Felodipine sustained release tablets (trade name: plendil®) |
Hypertension | Overseas Pharmaceuticals, Ltd. | October 28, 2022 | Phase 1 |
| NCT01238705 | Unknown | Drug: Felodipine add Irbesartan | Hypertension Sexual Dysfunction |
LanZhou University | April 2008 | Phase 4 |
| NCT00742066 | Unknown | Drug: Felodipine Drug: Irbesartan |
Hypertension Insulin Resistance |
Maastricht University Medical Center |
March 2008 | Not Applicable |
| NCT05258448 | Recruiting | Other: Chemoradiotherapy | Cardiac Toxicity Lung Cancer Stage III |
Odense University Hospital | August 2015 | |
| NCT05788159 | Not yet recruiting | Drug: Lacosamide Tablets | Epilepsy | Overseas Pharmaceuticals, Ltd. | April 1, 2023 | Phase 1 |
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