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Fendiline (hydrochloride) (CAS 13636-18-5) LS-H135

Alpha 2-adrenergic receptor antagonist
LS-H135-1 / 1 g / $175
LS-H135-5 / 5 g / $195
USA Shipment Only
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Description: Fendiline is an alpha 2-adrenergic receptor antagonist (Kd = 2.6 µM) and an L-type calcium channel blocker (IC50 = 17 µM) well-known for its coronary vasodilator effects. Fendiline has recently been reported to inhibit K-Ras plasma membrane localization (IC50 = 9.64 µM), which prevents K-Ras signal transduction and blocks the proliferation of K-Ras-transformed tumor cells. H135_ChemicalStructureImage.png
γ-phenyl-N-(1-phenylethyl)-benzenepropanamine, monohydrochloride
 
biochemical, chemical, antagonist
LS-H135
13636-18-5
C23H25N • HCl
≥95%
A crystalline solid
0
CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3.Cl
InChI=1S/C23H25N.ClH/c1-19(20-11-5-2-6-12-20)24-18-17-23(21-13-7-3-8-14-21)22-15-9-4-10-16-22;/h2-16,19,23-24H,17-18H2,1H3;1H
NJXWZWXCHBNOOG-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: ADRA2A related products

Usage Information

Fendiline (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the fendiline (hydrochloride) in the solvent of choice. Fendiline (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of fendiline (hydrochloride) in these solvents is approximately 15, 30, and 20 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of fendiline (hydrochloride) can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of fendiline (hydrochloride) in PBS, pH 7.2, is approximately 0.1 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Motulsky, H.J., Snavely, M.D., Hughes, R.J., et al. Interaction of verapamil and other calcium channel blockers with α1- and α2-adrenergic receptors. Circ. Res. 52(2), 226-231 (1983).
  2. Nawrath, H., Klein, G., Rupp, J., et al. Open state block by fendiline of L-type Ca++ channels in ventricular myocytes from rat heart. J. Pharmacol. Exp. Ther. 285(2), 546-552 (1998).
  3. Tripathi, O., Schreibayer, W., and Tritthart, H.A. Fendiline inhibits L-type calcium channels in guinea-pig ventricular myocytes: A whole-cell patch-clamp study. Br. J. Pharmacol. 108(4), 865-869 (1993).
  4. Csik, V., Szekeres, L., and Udvary, E. Comparison of two calcium antagonists, verapamil and fendiline, in an experimental model of myocardial ischaemia mimicking classical angina on effort. Br. J. Pharmacol. 79(1), 37-43 (1983).
  5. van der Hoven, D., Cho, K.-J., Ma, X., et al. Fendiline inhibits K-Ras plasma membrane localization and blocks K-Ras signal transmission. Mol. Cell. Biol. 33(2), 237-251 (2013).

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