An L-type calcium channel inhibitor
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Labeled Version(s)
30123(±)-Felodipine-d5
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Felodipine

Item No. 17535

Technical Information
Formal Name
4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid, 3-ethyl 5-methyl ester
CAS Number
72509-76-3
Synonyms
  • H 154/82
Molecular Formula
C18H19Cl2NO4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 20 mg/ml
λmax
236, 360 nm
SMILES
CC1=C(C(C(C(OCC)=O)=C(N1)C)C2=C(C(Cl)=CC=C2)Cl)C(OC)=O
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
InChi Key
RZTAMFZIAATZDJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Felodipine is an inhibitor of L-type calcium channels.1 It induces relaxation of precontracted isolated porcine coronary artery segments (EC50 = 0.15 nM), which highly express L-type calcium channels.2 Felodipine is selective for L-type calcium channels over N-, R-, and P/Q-type channels at 10 µM, as well as the T-type Cav3.2 channel (IC50 = 6.8 µM).1,3 Felodipine preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC50s = 33.9 and 3,981 nM, respectively).4 It decreases mean arterial blood pressure and total peripheral resistance in a rabbit model of hypertension induced by renal artery ligation when administered intravenously at doses of 30 and 100 nmol/kg.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Furukawa, T., Yamakawa, T., Midera, T., et alSelectivities of dihydropyridine derivatives in blocking Ca2+ channel subtypes expressed in Xenopus oocytes. J. Pharmacol. Exp. Ther. 291(2), 464-473 (1999).

    2. Johnson, J.D., and Fugman, D.A. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J. Pharmacol. Exp. Ther. 226(2), 330-334 (1983).

    3. Perez-Reyes, E., Van Deusen, A.L., and Vitko, I. Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: Block by antihypertensives, antiarrhythmics, and their analogs. J. Pharmacol. Exp. Ther. 328(2), 621-627 (2009).

    4. Ljung, B. Vascular selectivity of felodipine: Experimental pharmacology. J. Cardiovasc. Pharmacol. 15(Suppl 4), S11-S16 (1990).

    5. Bolt, G.R., and Saxena, P.R. Acute systemic and regional hemodynamic effects of felodipine, a new calcium antagonist, in conscious renal hypertensive rabbits. J. Cardiovasc. Pharmacol. 6(4), 707-712 (1984).