1. GPCR/G Protein
    Metabolic Enzyme/Protease
    Apoptosis
  2. Angiotensin Receptor
    Neprilysin
    Apoptosis
  3. LCZ696

LCZ696 (Synonyms: Sacubitril/Valsartan)

製品番号: HY-18204A 純度: 99.99% ee.: 99.99%
取扱説明書

LCZ696 (Sacubitril/Valsartan), comprised Valsartan (an ARB) and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. LCZ696 ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.

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LCZ696 構造式

LCZ696 構造式

CAS 番号 : 936623-90-4

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 105 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 190 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

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製品説明

LCZ696 (Sacubitril/Valsartan), comprised Valsartan (an ARB) and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure[1][2][3]. LCZ696 ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis[4].

IC50 & Target

Angiotensin receptor-neprilysin[1]

体外実験

LCZ696 (1-30 µM; 0.5 hours) inhibits HG-treated H9C2 cells apoptosis in an experimental model of Diabetic cardiomyopathy (DCM)[4].
LCZ696 (1-30 µM; 0.5 hours) increases the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2 in HG-treated H9C2 cells[4].

Apoptosis Analysis[4]

Cell Line: HG-treated H9C2 cells
Concentration: 1, 10, or 30 µM
Incubation Time: 0.5 hours
Result: Inhibited HG-treated H9C2 cells apoptosis.

Western Blot Analysis[4]

Cell Line: HG-treated H9C2 cells
Concentration: 1, 10, or 30 µM
Incubation Time: 0.5 hours
Result: Increased the expression level of cleaved caspase-3 and the ratio of Bax/Bcl-2.
体内実験

LCZ696 (perorally; 68 mg/kg for 4 weeks) significantly exhibits small weights and reduces interstitial fibrosis both in the noninfarct zone and peri-infarct zone[2].

Animal Model: Adult 6- to 8-week-old male Sprague-Dawley rats (220-250 g body weight) [2]
Dosage: 68 mg/kg
Administration: Perorally; for 4 weeks
Result: Exhibited small weights and reduced interstitial fibrosis both in the noninfarct zone and peri-infarct zone.
臨床実験
分子量

957.99

分子式

C₄₈H₆₀N₆Na₃O₁₀.₅

CAS 番号

936623-90-4

SMILES

O=C(CCC(O[Na])=O)N([[email protected]](CC(C=C1)=CC=C1C2=CC=CC=C2)C[[email protected]@H](C)C(OCC)=O)[H].O=C(O[Na])[[email protected]@H](N(C(CCCC)=O)CC3=CC=C(C4=CC=CC=C4C5=NN=NN5[Na])C=C3)C(C)C.[2.5H2O]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (104.39 mM)

H2O : ≥ 50 mg/mL (52.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0439 mL 5.2193 mL 10.4385 mL
5 mM 0.2088 mL 1.0439 mL 2.0877 mL
10 mM 0.1044 mL 0.5219 mL 1.0439 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.99% ee.: 99.99%

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LCZ696Sacubitril/ValsartanLCZ 696LCZ-696Angiotensin ReceptorNeprilysinApoptosisNeutral endopeptidaseNEPCluster of differentiation 10CD10 Inhibitorinhibitorinhibit

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製品名:
LCZ696
製品番号:
HY-18204A
数量:
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