Fendiline (hydrochloride) |
| Catalog No.GC18086 |
α2-adrenergic receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13636-18-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 13636-18-5 | SDF | |
| Chemical Name | γ-phenyl-N-(1-phenylethyl)-benzenepropanamine, monohydrochloride | ||
| Canonical SMILES | CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3.Cl | ||
| Formula | C23H25N • HCl | M.Wt | 351.9 |
| Solubility | ≥ 30mg/mL in DMSO, 20 mg/ml in DMF, 15 mg/ml in Ethanol, PBS (pH 7.2): 0.1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8417 mL | 14.2086 mL | 28.4172 mL |
| 5 mM | 0.5683 mL | 2.8417 mL | 5.6834 mL |
| 10 mM | 0.2842 mL | 1.4209 mL | 2.8417 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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