FENDILINE HYDROCHLORIDE
- CAS No.
- 13636-18-5
- Chemical Name:
- FENDILINE HYDROCHLORIDE
- Synonyms
- hk137;Sensit;difmecor;Fendilar;Fendiline HCl;FENDILINE HYDROCHLORIDE;N-(3,3-Diphenylpropyl)-α-methylbenzylamine;(3,3-diphenylpropyl)(1-phenylethyl)ammonium chloride;n-(1-phenylethyl)-3,3-diphenylpropylaminehydrochloride;N-(3,3-Diphenylpropyl)-α-methylbenzylamine hydrochloride
- CBNumber:
- CB1186062
- Molecular Formula:
- C23H26ClN
- Molecular Weight:
- 351.91
- MDL Number:
- MFCD00079301
- MOL File:
- 13636-18-5.mol
| Melting point | 204-205℃ |
|---|---|
| solubility | Soluble in ethanol. |
| form | Powder |
| FDA UNII | HEM3Z10IIK |
FENDILINE HYDROCHLORIDE price More Price(12)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Alfa Aesar | J63254 | Fendiline hydrochloride | 13636-18-5 | 5g | $131.65 | 2024-03-01 | Buy |
| Cayman Chemical | 17295 | Fendiline (hydrochloride) ≥95% | 13636-18-5 | 1g | $34 | 2024-03-01 | Buy |
| Cayman Chemical | 17295 | Fendiline (hydrochloride) ≥95% | 13636-18-5 | 5g | $92 | 2024-03-01 | Buy |
| Tocris | 6407 | Fendiline hydrochloride ≥98%(HPLC) | 13636-18-5 | 10 | $49 | 2021-12-16 | Buy |
| Tocris | 6407 | Fendiline hydrochloride ≥98%(HPLC) | 13636-18-5 | 50 | $204 | 2021-12-16 | Buy |
FENDILINE HYDROCHLORIDE Chemical Properties,Uses,Production
Originator
Sensit,Thiemann,W. Germany,1974
Uses
Fendiline is an α2-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.
Uses
Antianginal;Ca++ channel activator
Uses
Fendiline hydrochloride is used as a calcium channel blocker.
Manufacturing Process
21.13 grams of γ,γ-diphenyl-propylamine and 12.01 grams of acetophenone
are hydrogenated in 200 ml of methanol at 55°C and a pressure of 10
atmospheres in the presence of palladium charcoal. On filtration of the
catalyst the solution is concentrated and the remainder is distilled in vacuo at
a pressure of 0.3 Hg mm. The main distillate is collected at 206° to 210°C.
25.38 grams of N-[1'-phenylethyl-(1')]-1,1-diphenyl-propyl-(3)-amine are
obtained.
The product is dissolved in 134 ml of 96% ethanol whereupon 26.8 ml of
concentrated hydrochloric acid and 201 ml of water are added while cooling
with ice-water. The precipitate is filtered off and dried in vacuo at 100°C.
22.98 grams of N-[1'-phenylethyl)-(1')]-1,1-diphenyl-propyl-(3)-amine
hydrochloride are obtained. MP 200° to 201°C. On recrystallization from 285
ml of a 2:1 mixture of water and 96% ethanol the melting point remains
unchanged.
Therapeutic Function
Coronary vasodilator
Biological Activity
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].
storage
Store at +4°C
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.
FENDILINE HYDROCHLORIDE Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9348 | 55 |
| Shanghai Zheyan Biotech Co., Ltd. | 18017610038 | zheyansh@163.com | CHINA | 3620 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| 3B Pharmachem (Wuhan) International Co.,Ltd. | 821-50328103-801 18930552037 | 3bsc@sina.com | China | 15848 | 69 |
| Tianjin heowns Biochemical Technology Co., Ltd. | 400 638 7771 | sales@heowns.com | China | 14443 | 57 |
| Beijing HuaMeiHuLiBiological Chemical | 010-56205725 | waley188@sohu.com | China | 12338 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |