Sacubitril/valsartan (LCZ696)

製品コードS7678 バッチS767801

化学情報

	Synonyms	Sacubitril, Valsartan	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₉N₅O₃.C₂₄H₂₉NO₅.5/2H₂O.3Na
	分子量	915.98	CAS No.	936623-90-4
Solubility (25°C)*	体外	DMSO	100 mg/mL warmed with 50ºC water bath (109.17 mM)
		Water	100 mg/mL warmed with 50ºC water bath (109.17 mM)
		Ethanol	100 mg/mL warmed with 50ºC water bath (109.17 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
in vivo	In double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity, LCZ696 (60 mg/kg p.o.) induces a dose-dependent and long-lasting reduction in mean arterial pressure (MAP), and stimulates a rapid and dose-dependent augmentation of plasma ANP immunoreactivity. ^[1] In rat myocardial infarction (MI) model, LCZ696 (68 mg/kg p.o.) attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. ^[2]

製品説明

Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

in vivo

In double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity, LCZ696 (60 mg/kg p.o.) induces a dose-dependent and long-lasting reduction in mean arterial pressure (MAP), and stimulates a rapid and dose-dependent augmentation of plasma ANP immunoreactivity. ^[1] In rat myocardial infarction (MI) model, LCZ696 (68 mg/kg p.o.) attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. ^[2]

プロトコル(参考用のみ)

動物実験	動物モデル	Double-transgenic rats overexpressing human renin and angiotensinogen and plasma atrial natriuretic peptide immunoreactivity
	投薬量	~60 mg/kg
	投与方法	p.o.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , J Mol Cell Cardiol, 2017, 108:138-148]

: Data from [Data independently produced by , , RSC Adv, 2017, doi:10.1039/C7RA01404J]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

LCZ696 (sacubitril/valsartan) inhibits pulmonary hypertension induced right ventricular remodeling by targeting pyruvate dehydrogenase kinase 4 [ Biomed Pharmacother, 2023, 162:114569]	PubMed: 37001183
Sacubitril/valsartan alleviates sepsis-induced acute lung injury via inhibiting GSDMD-dependent macrophage pyroptosis in mice [ FEBS J, 2023, 290(8):2180-2198]	PubMed: 36471663
Sacubitril Valsartan Enhances Cardiac Function and Alleviates Myocardial Infarction in Rats through a SUV39H1/SPP1 Axis [ Oxid Med Cell Longev, 2022, 2022:5009289]	PubMed: 36193085
Sacubitril Valsartan Enhances Cardiac Function and Alleviates Myocardial Infarction in Rats through a SUV39H1/SPP1 Axis [ Oxid Med Cell Longev, 2022, 2022:5009289]	PubMed: 36193085
Sacubitril/valsartan reduces endoplasmic reticulum stress in a rat model of doxorubicin-induced cardiotoxicity [ Arch Toxicol, 2022, 96(4):1065-1074]	PubMed: 35152301
Direct actions of dapagliflozin and interactions with LCZ696 and spironolactone on cardiac fibroblasts of patients with heart failure and reduced ejection fraction [ ESC Heart Fail, 2022, 10.1002/ehf2.14186]	PubMed: 36303443
Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension [ Cardiovasc Res, 2021, 117(5):1391-1401]	PubMed: 32653925
LCZ696 Possesses a Protective Effect Against Homocysteine (Hcy)-Induced Impairment of Blood-Brain Barrier (BBB) Integrity by Increasing Occludin, Mediated by the Inhibition of Egr-1 [ Neurotox Res, 2021, 10.1007/s12640-021-00414-1]	PubMed: 34542838
LCZ696 improves cardiac function via alleviating Drp1-mediated mitochondrial dysfunction in mice with doxorubicin-induced dilated cardiomyopathy. [Xia Y, et al. J Mol Cell Cardiol, 2017, 108:138-148]	PubMed: 28623750
A metabolomics approach to profiling the cardioprotective effect of LCZ696, an angiotensin receptor-neprilysin inhibitor, on ischemia induced heart failure† [Yan Xia, et al. RSC Adv, 2017, 10.1039/C7RA01404J]

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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