Felodipine | CAS#72509-76-3 | calcium channel blocker

MedKoo Cat#: 317864 | Name: Felodipine

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Felodipine is a calcium channel blocker (calcium antagonist), used to control hypertension. Felodipine prevents calcium from being released within the muscle cells of the small arteries and thereby causes the muscles to relax and the arteries to dilate or expand. Dilation of arteries reduces blood pressure. Felodipine has little or no effect on the muscles of veins or the heart. Felodipine was approved by the FDA in 1991.

Chemical Structure

Felodipine

CAS#72509-76-3

Theoretical Analysis

MedKoo Cat#: 317864

Name: Felodipine

CAS#: 72509-76-3

Chemical Formula: C18H19Cl2NO4

Exact Mass: 383.0691

Molecular Weight: 384.25

Elemental Analysis: C, 56.26; H, 4.98; Cl, 18.45; N, 3.65; O, 16.66

Price and Availability

Size	Price	Availability
1g	USD 250.00	2 Weeks
2g	USD 350.00	2 Weeks
5g	USD 650.00	2 Weeks
10g	USD 950.00	2 Weeks

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Related CAS #

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Synonym

Felodipine, Agon, Felo-Puren, Felobeta, Felocor, Felodipin, Felodur Felogamma, Fensel, Flodil, Modip, Munobal, Perfudal, Plendil, Renedil; H 154/82; H154/82; H-154/82; NSC-760343; NSC760343; NSC 760343

IUPAC/Chemical Name

3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

InChi Key

RZTAMFZIAATZDJ-UHFFFAOYSA-N

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

SMILES Code

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OCC

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist.

In vitro activity:

Therefore, to test whether these concentrations were likely to be inducing autophagy, this study examined the effects of low concentrations (50 and 100 nM) of felodipine in cultured primary neurons. Indeed, these concentrations increased the numbers of autolysosomes (suggesting increased autophagic flux) and significantly reduced the percentages of neurons with mutant huntingtin exon 1 aggregates (Fig. 4b, c). Reference: Nat Commun. 2019; 10: 1817. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6472390/

In vivo activity:

Treatment with felodipine significantly downregulated the genes associated with osteoclast differentiation. RNA-sequencing and western blotting suggested that felodipine could inhibit bone resorption by suppressing MAPK pathway phosphorylation. Moreover, micro-CT scanning and histological analysis in an ovariectomy (OVX)-induced bone-loss mouse model indicated that felodipine might be a potent drug for preventing osteoporotic fractures. Reference: Exp Cell Res. 2020 Feb 15;387(2):111800. https://pubmed.ncbi.nlm.nih.gov/31877305/

	Solvent	mg/mL	mM
Solubility
	DMSO	61.4	159.69
	DMSO:PBS (pH 7.2) (1:3)	0.3	0.65
	DMF	30.0	78.07
	Ethanol	43.5	113.13

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Siddiqi FH, Menzies FM, Lopez A, Stamatakou E, Karabiyik C, Ureshino R, Ricketts T, Jimenez-Sanchez M, Esteban MA, Lai L, Tortorella MD, Luo Z, Liu H, Metzakopian E, Fernandes HJR, Bassett A, Karran E, Miller BL, Fleming A, Rubinsztein DC. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing. Nat Commun. 2019 Apr 18;10(1):1817. doi: 10.1038/s41467-019-09494-2. Erratum in: Nat Commun. 2019 Jun 4;10(1):2530. PMID: 31000720; PMCID: PMC6472390. 2. Qi J, Zheng JB, Ai WT, Yao XW, Liang L, Cheng G, Shou XL, Sun CF. Felodipine inhibits ox-LDL-induced reactive oxygen species production and inflammation in human umbilical vein endothelial cells. Mol Med Rep. 2017 Oct;16(4):4871-4878. doi: 10.3892/mmr.2017.7181. Epub 2017 Aug 7. PMID: 28791379. 3. Zhang S, Li H, Tang H, Huo S, Nie B, Qu X, Yue B. Felodipine blocks osteoclast differentiation and ameliorates estrogen-dependent bone loss in mice by modulating p38 signaling pathway. Exp Cell Res. 2020 Feb 15;387(2):111800. doi: 10.1016/j.yexcr.2019.111800. Epub 2019 Dec 23. PMID: 31877305. 4. Tanaka KI, Niino T, Ishihara T, Takafuji A, Takayama T, Kanda Y, Sugizaki T, Tamura F, Kurotsu S, Kawahara M, Mizushima T. Protective and therapeutic effect of felodipine against bleomycin-induced pulmonary fibrosis in mice. Sci Rep. 2017 Jun 13;7(1):3439. doi: 10.1038/s41598-017-03676-y. PMID: 28611390; PMCID: PMC5469778.

In vitro protocol:

In vivo protocol:

1. Zhang S, Li H, Tang H, Huo S, Nie B, Qu X, Yue B. Felodipine blocks osteoclast differentiation and ameliorates estrogen-dependent bone loss in mice by modulating p38 signaling pathway. Exp Cell Res. 2020 Feb 15;387(2):111800. doi: 10.1016/j.yexcr.2019.111800. Epub 2019 Dec 23. PMID: 31877305. 2. Tanaka KI, Niino T, Ishihara T, Takafuji A, Takayama T, Kanda Y, Sugizaki T, Tamura F, Kurotsu S, Kawahara M, Mizushima T. Protective and therapeutic effect of felodipine against bleomycin-induced pulmonary fibrosis in mice. Sci Rep. 2017 Jun 13;7(1):3439. doi: 10.1038/s41598-017-03676-y. PMID: 28611390; PMCID: PMC5469778.

1: Uesawa Y, Takeuchi T, Mohri K. Publication bias on clinical studies of pharmacokinetic interactions between felodipine and grapefruit juice. Pharmazie. 2010 May;65(5):375-8. Review. PubMed PMID: 20503932. 2: Cvetković RS, Plosker GL. Ramipril/felodipine extended-release fixed-dose combination: a review of its use in the management of essential hypertension. Drugs. 2005;65(13):1851-68. Review. PubMed PMID: 16114982. 3: Haria M, Plosker GL, Markham A. Felodipine/metoprolol: a review of the fixed dose controlled release formulation in the management of essential hypertension. Drugs. 2000 Jan;59(1):141-57. Review. PubMed PMID: 10718104. 4: Little WC, Cheng CP, Elvelin L, Nordlander M. Vascular selective calcium entry blockers in the treatment of cardiovascular disorders: focus on felodipine. Cardiovasc Drugs Ther. 1995 Oct;9(5):657-63. Review. PubMed PMID: 8573548. 5: Dahlöf B, Andersson OK. A felodipine-metoprolol extended-release tablet: its properties and clinical development. J Hum Hypertens. 1995 Jul;9 Suppl 2:S43-7. Review. PubMed PMID: 7562899. 6: Trenkwalder P, Elmfeldt D. Improving the therapeutic balance between efficacy and tolerability in antihypertensive drugs--the rationale and benefits of combining felodipine and metoprolol. J Hum Hypertens. 1995 Jul;9 Suppl 2:S37-42. Review. PubMed PMID: 7562898. 7: Gradman AH. The evolving role of calcium channel blockers in the treatment of angina pectoris: focus on felodipine. Can J Cardiol. 1995 Apr;11 Suppl B:14B-21B. Review. PubMed PMID: 7728649. 8: Purcell H, Coats A. Structural changes in hypertension, the potential for their prevention, arrest and reversal: a focus on felodipine. Br J Clin Pract. 1994 Nov-Dec;48(6):311-6. Review. PubMed PMID: 7848795. 9: Walton T, Symes LR. Felodipine and isradipine: new calcium-channel-blocking agents for the treatment of hypertension. Clin Pharm. 1993 Apr;12(4):261-75. Review. PubMed PMID: 8458178. 10: Gradman AH. Treatment of hypertension with felodipine in patients with concomitant diseases. Clin Cardiol. 1993 Apr;16(4):294-301. Review. PubMed PMID: 8458109. 11: Faulds D, Sorkin EM. Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in older patients. Drugs Aging. 1992 Sep-Oct;2(5):374-88. Review. PubMed PMID: 1392220. 12: Todd PA, Faulds D. Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders. Drugs. 1992 Aug;44(2):251-77. Review. PubMed PMID: 1382018. 13: Elmfeldt D, Nordlander M, Edgar B. Renal effects of felodipine--a review. Kidney Int Suppl. 1992 May;36:S54-60. Review. PubMed PMID: 1614069. 14: DeQuattro V. Efficacy and safety of felodipine, a new dihydropyridine calcium channel blocker, in elderly hypertensive patients. Clin Exp Hypertens A. 1992;14(6):965-87. Review. PubMed PMID: 1424224. 15: Dunselman PH, Edgar B. Felodipine clinical pharmacokinetics. Clin Pharmacokinet. 1991 Dec;21(6):418-30. Review. PubMed PMID: 1782737. 16: Yedinak KC, Lopez LM. Felodipine: a new dihydropyridine calcium-channel antagonist. DICP. 1991 Nov;25(11):1193-206. Review. PubMed PMID: 1763537. 17: Lorimer AR, Pringle SD. The safety of felodipine. J Cardiovasc Pharmacol. 1990;15 Suppl 4:S85-9. Review. PubMed PMID: 1693736. 18: Morgan TO. A review of the antihypertensive effects of felodipine alone or in combination. J Cardiovasc Pharmacol. 1990;15 Suppl 4:S76-84. Review. PubMed PMID: 1693735. 19: Reid JL. Dose-plasma concentration--effect relationship of felodipine in essential hypertension: a review. J Cardiovasc Pharmacol. 1990;15 Suppl 4:S50-6. Review. PubMed PMID: 1693728. 20: Lund-Johansen P. Hemodynamic effects of felodipine in hypertension: a review. J Cardiovasc Pharmacol. 1990;15 Suppl 4:S34-9. Review. PubMed PMID: 1693723.