(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide
Aliskiren
CAS: 173334-57-1
Molecular Formula: C30H53N3O6
(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide - Names and Identifiers
(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide - Physico-chemical Properties
| Molecular Formula | C30H53N3O6 |
| Molar Mass | 551.76 |
| Density | 1.067±0.06 g/cm3(Predicted) |
| Melting Point | 98-99 °C |
| Boling Point | 748.4±60.0 °C(Predicted) |
| Flash Point | 417.1°C |
| Vapor Presure | 1.12E-24mmHg at 25°C |
| pKa | 9.49(at 25℃) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Use | Renin inhibitors |
(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.812 ml | 9.062 ml | 18.123 ml |
| 5 mM | 0.362 ml | 1.812 ml | 3.625 ml |
| 10 mM | 0.181 ml | 0.906 ml | 1.812 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.362 ml |
Last Update：2024-01-02 23:10:35
(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide - Reference Information
| overview | alicron (English Aliskiren) is a second-generation renin inhibitor that acts on the renin angiotensin aldosterone system (RAS) The first rate limiting step. At present, all research data show that aliclan antihypertensive therapy has good safety and effectiveness, few side effects, long half-life, and convenient to take once a day. Now it has entered phase III clinical practice and is expected to become the first oral renin inhibitor for the treatment of hypertension and other cardiovascular diseases and nephropathy. Compared with ACEI, alik can reduce angiotensin II production more effectively. Clinical trials have also confirmed that the combination of alik and ARB has a synergistic effect on the inhibition of RAS and can eliminate the effect of ARB-induced angiotensin II accumulation. A phase II clinical trial conducted in Ireland (multi-center, double-blind, positive controlled trial) confirmed for the first time that alik can effectively reduce blood pressure levels in patients with mild to moderate hypertension. The 8-week expanded sample phase III clinical trial increased the placebo control and compared with irbesartan, which further confirmed the efficacy of alik for patients with mild to moderate hypertension, and confirmed that the antihypertensive effect of alik was increased in a dose-dependent manner below the dose of 300mg. Arikron does not produce reflex tachycardia and does not affect heart function; the antihypertensive effect is renin-dependent, so large-dose administration will only prolong the action time and will not cause a sudden drop in blood pressure. Similar to ARB, there was no significant difference in the incidence of aliceram adverse reactions compared with placebo. US FDA approved Novartis's Allikiren (aliskiren) tablets (trade name: Tekturna) for the treatment of hypertension. Dose specification: 150mg/tablet, 300mg/tablet. Alykiren is a new molecular entity, which is the first hypertension drug approved by the US FDA to directly inhibit the renal enzyme renin that causes elevated blood pressure. It is predicted that the sales of alicron will reach US $2 billion by 2015. |
| market situation | alicron is the first new, highly effective and orally effective human renin non-peptide inhibitor, with a long chain structure similar to the peptide chain structure of natural renin, with good renin inhibitory activity and ic50 reaching nanomole. Good physical and chemical properties make it have better oral absorption properties and a certain degree of bioavailability. aliskiren is a second-generation renin inhibitor developed by Novartis to act on the renin angiotensin aldosterone system (ras). U.S. fda approved aliskiren listing in May 2007. alik was approved by fda and the European Union in 2007, and is the first new compound approved by fda for the treatment of hypertension in the past 10 years. In 2009, Japan also approved the drug to join the Japanese market. The compound patent expires in 2015, and Novartis has successively applied for about 20 compound route patent protection. alik is a new molecular entity, which is the first hypertension drug approved by fda in the United States to directly inhibit renin, a renal enzyme that causes elevated blood pressure. Aliciren is a second-generation renin inhibitor. Aliskiren is a new generation of non-peptide renin blockers. It can block the RAS system in the first link, reduce renin activity, and reduce the production of AngII and aldosterone. It does not affect the metabolism of bradykinin and prostaglandin, and plays a role in lowering blood pressure and treating cardiovascular diseases. From the current research, aliskiren is a powerful, highly selective, orally effective and long-acting new generation of antihypertensive drugs. The drug acts on renin-dependent, so increasing the dose will only prolong the time and will not cause a sudden drop in blood pressure. Similar to ARB (losartan, telmisartan), the incidence of adverse reactions is compared with placebo There is no significant difference in the group. |
| patent status | this product has a compound patent, and the protection period will expire in April 2015. Aliskiren was approved by FDA and the European Union in 2007. It is the first new compound approved by FDA for the treatment of hypertension in the past 10 years. In 2009, Japan also approved the drug to join the Japanese market. The compound patent expires in 2015, and Novartis has successively applied for about 20 compound synthesis route patent protection, as well as other types of patents. U.S. compound patent (authorization) China 95105037.0 compound patent (authorization) 1995.4.17 |
| biological activity | Aliskiren is a renin inhibitor with antihypertensive activity. |
| target | TargetValue Renin () |
| Target | Value |
| use | renin inhibitor |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov provided (external link) |
Last Update：2024-04-09 19:05:03
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View History
(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide
3-amino-N-(4-chloro-2-fluorophenyl)-6-methyl-5,6,7,8-tetrahydrothieno[2,3-b][1,6]naphthyridine-2-carboxamide
5-(1-Piperazinyl)-2-benzofurancarboxamide hydrochloride
2-Amino-4,6-difluorobenzyl Alcohol
铬鞣剂
2H-Indol-2-one, 1,3-dihydro-3-[2-(2-methylphenyl)-6-oxothiazolo[3,2-b][1,2,4]triazol-5(6H)-ylidene]-1-propyl-
5124-91-4
113106-71-1
312317-55-8
(5,6,7,8-Tetrahydroquinolin-8-yl)methanamine
3-amino-N-(4-chloro-2-fluorophenyl)-6-methyl-5,6,7,8-tetrahydrothieno[2,3-b][1,6]naphthyridine-2-carboxamide
5-(1-Piperazinyl)-2-benzofurancarboxamide hydrochloride
2-Amino-4,6-difluorobenzyl Alcohol
铬鞣剂
2H-Indol-2-one, 1,3-dihydro-3-[2-(2-methylphenyl)-6-oxothiazolo[3,2-b][1,2,4]triazol-5(6H)-ylidene]-1-propyl-
5124-91-4
113106-71-1
312317-55-8
(5,6,7,8-Tetrahydroquinolin-8-yl)methanamine