FelodipineA 1,4-dihydropyridine antagonist and calcium channel protein inhibitor

Felodipine (CAS 72509-76-3)

Felodipine | CAS 72509-76-3 is rated 5.0 out of 5 by 1.
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Synonym: Plendil
Application: A 1,4-dihydropyridine antagonist and calcium channel protein inhibitor
CAS Number: 72509-76-3
Molecular Weight: 384.3
Molecular Formula: C18H19Cl2NO4
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Felodipine is a 1,4-dihydropyridine small molecule antagonist and calcium channel protein inhibitor. Antagonism of the vascular L-type (long-lasting) calcium channel decreases intracellular calcium concentration, softening the tone of vascular tissue and decreasing the peripheral resistance upon the blood stream, effectively decreasing systemic arterial blood pressure without affecting myocardial contractility. 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

1. Ljung, B. 1990. J. Cardiovasc. Pharmacol. 15: S11-S16. PMID: 1693715
2. Blychert, E. 1992. Blood Press Suppl. 2: 1-30. PMID: 1343111
3. Little, W.C. and Cheng, C.P. 1994. Drugs. 47: 41-45. PMID: 7523061
4. Gradman, A.H. 1995. Can J Cardiol. 11: 14B-21B. PMID: 7728649
5. Little, W.C., et al. 1995. Cardiovasc Drugs Ther. 9: 657-663. PMID: 8573548
6. Palma-Gámiz, J.L. 1997. Cardiology. 88: 39-46. PMID: 9118167
7. Sarsero, D., et al. 1998. Br. J. Pharmacol. 125: 109-119. PMID: 9776350
8. Hishikawa, K. and Lüscher, T.F. 1998. Hypertension. 32: 1011-1015. PMID: 9856965
9. Angus, J.A., et al. 2000. Clin. Exp. Pharmacol. Physiol. 27: 1019-1021. PMID: 11117223

Physical State :
Solid
Solubility :
Soluble in DMSO (>25 mg/ml), ethanol (20 mg/ml), methanol, chloroform, and acetone. Insoluble in water.
Storage :
Store at room temperature
Melting Point :
145° C
Boiling Point :
471.52° C at 760 mmHg
Density :
1.28
Refractive Index :
n20D 1.55
IC50 :
Calcium channel: IC50 = 1.45 nM (Cavia porcellus); Sodium channel protein type III alpha subunit: IC50 = 37000 nM (human); Sodium channel protein type I alpha subunit: IC50 = 37000 nM (human); Danio rerio: IC50 = 9210 nM
pK Values :
pKb: 2.73
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
US7968700
PubChem CID :
3333
Merck Index :
14: 3953
MDL Number :
MFCD00868316
SMILES :
CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C

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Certificate of Analysis

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Felodipine  Product Citations

See how others have used Felodipine. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23688559  Yu, DD. et al. 2013. Bioorg. Med. Chem. 21: 4266-78.

Citations 1 to 1 of 1 total

Is felodipine soluble in water?

Asked by: Maliha
Thank you for your question. Felodipine is insoluble in water.
Answered by: Technical Support
Date published: 2018-12-03
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Rated 5 out of 5 by from Hishikawa et al Hishikawa et al. (PubMed ID 9856965) found that Felodipine inhibited the production of free radicals by cytokines and glucose, exerting a vascular protective effect in human smooth muscle cells after induced inflammation. -SCBT Publication Review
Date published: 2015-05-30
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