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72509-76-3 (Felodipine)

1

Identification

Felodipine Felodipine
Name Felodipine
Formula C18H19Cl2NO4
MW 384.25
CAS No. 72509-76-3
EINECS
Smiles O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OCC
Synonyms Plendil;Renedil;Feloday; 3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
InChI 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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Introduction

Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. Target: Calcium Channel Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker (CCB)b.

Background Information

Felodipine is an L-type (CaV1), voltage-gated Ca2+ channels are plasma membrane protein.Felodipine is a DHP that acts as L-type, voltage-gated Ca2+ channel blocker that is selective over N-, R-, P/Q- and T-type channels. ......by Affix Scientific
Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM. ......by BOC Sciences
Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM. ......by Selleck Chemicals LLC
A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. ......by Target Molecule Corp.
L-type Ca2+ channel blocker that is selective over N-, R-, P/Q- and T-type channels. Displays high vascular selectivity; lowers arterial blood pressure without altering cardiac contractility. Antihypertensive. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Male Sprague-Dawley rats with approximately 5/6 renal ablation
Dosage 1 g/kg/day
Formulation Dissolved in DMSO, and diluted in saline
Administration Orally
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000012560

Storage condition

Up to one week at 4°C or six months at -20°C. by Affix Scientific
Store at +4°C by Tocris Bioscience Inc.

Solubility

DMSO 77 mg/mL; Water <1 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 77 mg/mL (200.39 mM); Ethanol72 mg/mL (187.37 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC
Soluble to 100 mM in DMSO and to 100 mM in ethanol by Tocris Bioscience Inc.
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Mechanism and Indication

Signaling Pathways Membrane Transporter/Ion Channel
Target Calcium Channel
Research Area Cardiovascular Disease
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Felodipine - Launched
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Safety Data of Felodipine

Hazard Symbols : Xn
Risk Statements : 22
Safety Statements : 36
RTECS : US7968700
WGKGermany : 3
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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
Affix Scientific 1g/USD1660(In stock) USA
Anhui Modern Chem-Pharm Co., Ltd. China
BOC Sciences 5g/USD298(In stock)
CHEMSCENE, LLC 10mg/USD85();50mg/USD209() USA
Changzhou Hengfeng Chemical Plant China
Changzhou Ruiming Pharmaceutical Co., Ltd. China
MedChemexpress Co., Ltd. 10mg/USD85();50mg/USD209() USA
Selleck Chemicals LLC 10mg/USD97(In stock);10mM/1mLIn DMSO/USD130(In stock);50mg/USD310(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD85();50mg/USD209() China
Target Molecule Corp. 2mg/USD36();10mg/USD65();50mg/USD165();100mg/USD268() USA
Tocris Bioscience Inc. USA
Zhejiang Wonderful Pharma & Chem Co., Ltd. China
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Related Products

Other Forms of 72509-76-3

Name CAS No Formula MW

Recommended Compounds in Calcium Channel

Name CAS No Formula MW
Lercanidipine (hydrochloride) 132866-11-6 C36H42ClN3O6 648.19
Amlodipine (maleate) 88150-47-4 C24H29ClN2O9 524.9481
Lercanidipine 100427-26-7 C36H41N3O6 611.73
Neomycin (sulfate) 1405-10-3 C23H48N6O17S 712.72
Tetracaine (hydrochloride) 136-47-0 C15H25ClN2O2 300.82
Nitrendipine 39562-70-4 C18H20N2O6 360.36
Manidipine 89226-50-6 C35H38N4O6 610.7
Chlorpromazine (hydrochloride) 69-09-0 C17H20Cl2N2S 355.33
Ibutilide (fumarate) 122647-32-9 C44H76N4O10S2 885.23
Flunarizine (dihydrochloride) 30484-77-6 C26H28Cl2F2N2 477.42
Lacidipine 103890-78-4 C26H33NO6 455.54
Cromolyn (sodium) 15826-37-6 C23H14Na2O11 512.33
Amlodipine 88150-42-9 C20H25ClN2O5 408.88
Nifedipine 21829-25-4 C17H18N2O6 346.33
Acetylcholine (chloride) 60-31-1 C7H16ClNO2 181.6604
Ranolazine 95635-55-5 C24H33N3O4 427.54
Nimodipine 66085-59-4 C21H26N2O7 418.44
Isradipine 75695-93-1 C19H21N3O5 371.39
Zonisamide (sodium) 68291-98-5 C8H7N2NaO3S 234.21
Zonisamide 68291-97-4 C8H8N2O3S 212.23

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

[1]. Johnson, J.D. and D.A. Fugman, Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther, 1983. 226(2): p. 330-4.

[2]. Rodler, S., et al., Ca(2+)-channel blockers modulate the expression of interleukin-6 and interleukin-8 genes in human vascular smooth muscle cells. J Mol Cell Cardiol, 1995. 27(10): p. 2295-302.

[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.

Protocol Reference

Ljung (1990) Vascular selectivity of felodipine: experimental pharmacology. J.Cardiovasc.Pharmacol. 15 S11. PMID: 1693715.

Furukawa et al (1999) Selectivities of dihydropyridine derivatives in blocking Ca2+ channel subtypes expressed in Xenopus oocytes. J.Pharmacol.Exp.Ther. 291 464. PMID: 10525060.

Furukawa et al (2005) Differential blocking action of dihydropyridine Ca2+ antagonists on a T-type Ca2+ channel (α1G) expressed in Xenopus oocytes. J.Cardiovasc.Pharmacol. 45 241. PMID: