Fendiline (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Fendiline is an α2-adrenergic receptor antagonist and L-type calcium channel blocker [1,2].
The α2 adrenergic receptor is a G protein-coupled receptor (GPCR). Until now, three different α2-receptor subtypes have been identified: α2A, α2B, and α2C. The α2-adrenergic receptor exists in vascular prejunctional terminals and inhibits the release of norepinephrine in a form of negative feedback. The α2 adrenergic receptor agonists produce diverse responses, including analgesia, sedation, anxiolysis, and sympatholysis [3]. L-type calcium channels are responsible for the excitation-contraction coupling of skeletal, cardiac muscle, smooth, and for aldosterone secretion in endocrine cells of the adrenal cortex [4].
Fendiline inhibited the activity of L-type Ca2+ channel blocker with the IC50 value of 17 μM [1]. Fendiline inhibited the activity of α2-adrenergic receptor with the Kd of 2.6 μM [2]. Fendiline significantly reduced nanoclustering of K-Ras and redistributed K-Ras from the plasma membrane to the endoplasmic reticulum (ER), Golgi apparatus, endosomes, and cytosol. Fendiline significantly inhibited signaling downstream of constitutively active K-Ras and endogenous K-Ras signaling in cells transformed by oncogenic H-Ras. Fendiline blocked the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras [5]. Fendiline inhibited K-Ras plasma membrane localization with an IC50 of 9.64 μM [5]. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials [6].
References:
[1] 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. British Journal of Pharmacology 108(4), 865-869 (1993).
[2] 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. Circulation Research 52(2), 226-231 (1983).
[3] Kamibayashi T, Maze M. Clinical uses of α2-adrenergic agonists[J]. The Journal of the American Society of Anesthesiologists, 2000, 93(5): 1345-1349.
[4] Lipscombe D. L-type calcium channels[J]. 2002.
[5] van der Hoeven D, Cho K, Ma X, et al. Fendiline inhibits K-Ras plasma membrane localization and blocks K-Ras signal transmission[J]. Molecular and cellular biology, 2013, 33(2): 237-251.
[6] Bayer R, Mannhold R. Fendiline: a review of its basic pharmacological and clinical properties[J]. Pharmatherapeutica, 1986, 5(2): 103-136.
Storage | Store at -20°C |
M.Wt | 351.9 |
Cas No. | 13636-18-5 |
Formula | C23H25N·HCl |
Solubility | insoluble in H2O; ≥16.6 mg/mL in DMSO; ≥2.34 mg/mL in EtOH with ultrasonic |
Chemical Name | γ-phenyl-N-(1-phenylethyl)-benzenepropanamine, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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