サクビトリルバルサルタンナトリウム水和物

サクビトリルバルサルタンナトリウム水和物 価格 もっと(4)

メーカー	製品番号	製品説明	CAS番号	包装	価格	更新時間	購入
富士フイルム和光純薬株式会社(wako)	W01COBQJ-8277	Lcz696	936623-90-4	250mg	￥82800	2018-12-26	購入
富士フイルム和光純薬株式会社(wako)	W01COBQJ-8277	Lcz696	936623-90-4	1g	￥208800	2018-12-26	購入
富士フイルム和光純薬株式会社(wako)	W01COBQJ-8277	Lcz696	936623-90-4	5g	￥630000	2018-12-26	購入
富士フイルム和光純薬株式会社(wako)	W01COBQV-6107	Lcz696	936623-90-4	100mg	￥176400	2018-12-26	購入

サクビトリルバルサルタンナトリウム水和物 化学特性,用途語,生産方法

効能

血圧降下薬

説明

LCZ696 is a dual angiotensin II receptor antagonist and neprilysin inhibitor that is a combination of the nonpeptide angiotensin II receptor antagonist valsartan and AHU377 , a prodrug of LBQ657 , which is an inhibitor of the zinc metallopeptidase neprilysin., LCZ696 (2-60 mg/kg) induces a dose-dependent decrease in mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension. Formulations containing LCZ696 are under clinical investigation for the treatment of mild to moderate hypertension and chronic heart failure.

作用機序

LCZ696 is a molecule that combines the moieties of valsartan and sacubitril (the neprilysin inhibitor) in a single substance. By inhibiting neprilysin, the degradation of natriuretic peptides, bradykinin, and other peptides is slowed. Hence, high circulating levels of natriuretic peptides enhance diuresis , natriuresis, myocardial relaxation, and anti-remodelling, on top of the ARB effects of valsartan.

臨床応用

LCZ696 (Novartis Pharmaceuticals), a first-in-class inhibitor of dualacting angiotensin-2 type-I receptor and neprilysin inhibitors, was developed as a molecule composed of molecular moieties of valsartan and neprilysin inhibitor prodrug AHU377 in a 1:1 ratio. Several phase 2 randomised clinical trials have been done or are underway in patients with hypertension. In a proof-of-concept randomised trial, LCZ696 was compared with valsartan in 1328 patients with mild-to-moderate hypertension, and provided fully additive reduction of blood pressure. No cases of angio-oedema were reported in the 8 week treatment period. This tolerance should be confirmed, particularly in black patients, for whom omapatrilat resulted in a higher occurrence of angio-oedema than in white patients. Indeed, in the proof-of-concept trial only about 8% of patients were black.

参考文献

1. McMurray, John J. V. et al. “Angiotensin-neprilysin inhibition versus enalapril in heart failure.” The New England journal of medicine 371 11 (2014):  993-1004. DOI: 10.1056/NEJMoa1409077
2. Gu, Jessie et al. “Pharmacokinetics and Pharmacodynamics of LCZ696, a Novel Dual‐Acting Angiotensin Receptor—Neprilysin Inhibitor (ARNi).” The Journal of Clinical Pharmacology 50 (2010): n. pag. DOI: 10.1177/0091270009343932
3. Langenickel, T.H., & Dole, W.P. (2012). Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure. Drug Discovery Today: Therapeutic Strategies, 9. DOI: 10.1016/J.DDSTR.2013.11.002
4. Suematsu, Yasunori et al. “LCZ696, an angiotensin receptor–neprilysin inhibitor, improves cardiac function with the attenuation of fibrosis in heart failure with reduced ejection fraction in streptozotocin‐induced diabetic mice.” European Journal of Heart Failure 18 (2016): n. pag. DOI: 10.1002/ejhf.474

サクビトリルバルサルタンナトリウム水和物 上流と下流の製品情報

原材料

準備製品

サクビトリルバルサルタンナトリウム水和物 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
Zibo Wei Bin Import & Export Trade Co. Ltd.	+86-0533-2091136 +8613864437655	ziboweibinmaoyi@163.com	China	100	58
ChemExpress	+86-021-58950125	info@chemexpress.com	China	555	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	8174	58
Hangzhou Hyper Chemicals Limited	+86-0086-57187702781 +8613675893055	info@hyper-chem.com	China	60	58
Ouhuang Engineering Materials (Hubei) Co., Ltd	+8617702722807	admin@hbouhuang.com	China	2991	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Nanjing Gold Pharmaceutical Technology Co. Ltd.	025-84209270 15906146951		CHINA	115	55
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55

936623-90-4(サクビトリルバルサルタンナトリウム水和物)キーワード:

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• 936623-90-4
• [(C24H29N5O3).(C24H29NO5).2.5(H2O).3Na]
• LCZ696 ENTRESTO TM
• LCZ696 Entresto
• 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoate
• Sacubitril mixture with Valsartan
• Cocrystal of Sacubitril and Valsartan
• (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)hexanamido)-3-methylbutanoic acid
• lcz696/Valsartan/sacubitril
• Sacubitril-Valsartan complex
• 3-(1-Biphenyl-4-ylMethyl-3-ethoxycarbonyl-1-butylcarbaMoyl)propionate-3'-Methyl-2'-(pentanoyl(2'-(tetrazol-5-ylate)biphenyl-4'-ylMethyl)aMino)butyrate
• LCZ696
• LCZ696 interMediate
• N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine, compd. with α-ethyl (αR,γS)-γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl[1,1'-biphenyl]-4-pentanoate, sodium salt, hydrate (2)
• Valsartan-sacubitril(LCZ696)
• sodium (S)-5-(4'-((N-(1-carboxylato-2-methylpropyl)pentanamido)methyl)-[1,1'-biphenyl]-2-yl)tetrazol-1-ide 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate
• LCZ696 (936623-90-4)
• Valsartan/Sacubitril (1:1)
• Entresto,Valsartan/sacubitril
• LCZ696 (Shakubi Qusarsartan)
• LCZ696;LCZ 696
• Entresto (sacubitril/valsartan) LCZ696
• Valsartan-Sacubitril sodium
• LCZ696 (Valsartan)
• LCA696
• Sacubitril Valsartan (LCZ696)
• Entresto（LCZ696）
• Sacubatro valsartan
• LCZ696 USP/EP/BP
• Secubitril
• Radix isatidis polysaccharides
• サクビトリルバルサルタンナトリウム水和物
• サクビトリルバルサルタンナトリウム水和物 (JAN)
• N-(1-オキソペンチル)-N-[[2′-(2H-テトラゾール-5-イル)-4-ビフェニリル]メチル]-L-バリン/(αR,γS)-γ-[(3-カルボキシ-1-オキソプロピル)アミノ]-α-メチル-4-ビフェニルペンタン酸α-エチル/ナトリウム/水和物,(2:2:6:5)
• LCZ-696