LCZ696
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LCZ696是第一类ARNi(血管紧张素受体脑啡肽酶抑制剂),由血管紧张素受体(AR)抑制剂valsartan的阴离子基团和用于心脏衰竭和高血压的前药AHU377,即脑啡肽酶抑制剂以1:1的比例组成。
血管紧张素受体是G蛋白偶联受体,它们介导肾素-血管紧张素系统的生物活性肽血管紧张素II的心血管和其它效应。脑啡肽酶是一种中性内肽酶,降解内源性血管活性肽,例如钠尿肽。脑啡肽酶的抑制会增加钠尿肽的浓度,从而有助于心脏,血管和肾脏的保护[1]。
在Sprague-Dawley大鼠中,LCZ696口服给药后通过对脑啡肽酶的抑制,从而剂量依赖地增加心钠素的免疫反应性。在高血压双转基因大鼠中,LCZ696引起平均动脉压剂量依赖地和持续性地下降。一个健康参与者、随机、双盲和安慰剂对照的研究证实,LCZ696同时诱导脑啡肽酶的抑制和AT1受体的阻断。LCZ696在人体中安全,耐受性良好[2] [3]。
参考文献:
1. McMurray JJ, Packer M, Desai AS et al. Angiotensin-neprilysin inhibition versus enalapril in heart failure. N Engl J Med. 2014 Sep 11;371(11):993-1004.
2. Gu J, Noe A, Chandra P, Al-Fayoumi S et al. Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14.
3. Langenickel TH, Dole WP. Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure, Drug Discov Today: Ther Strategies (2014),
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 956.99 |
Cas No. | 936623-90-4 |
Formula | C48H54N6Na3O8·2.5H2O |
Solubility | ≥45.05 mg/mL in DMSO; ≥11.28 mg/mL in H2O; ≥28.5 mg/mL in EtOH |
SDF | Download SDF |
Canonical SMILES | CCCCC(N([C@@](C([O-])=O)([H])C(C)C)CC1=CC=C(C2=CC=CC=C2C3=N[N-]N=N3)C=C1)=O.CCOC([C@](C[C@@](/N=C([O-])/CCC([O-])=O)([H])CC4=CC=C(C5=CC=CC=C5)C=C4)([H])C)=O.[3Na+].[2.5H2O] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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