AHU-377 hemicalcium salt
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Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AHU-377 hemicalcium salt是一种 AHU-377的半钙盐形式,是脑啡肽酶的抑制剂,IC50值为5 nM[1].
AHU-377和血管紧张素II AT1受体拮抗剂缬沙坦(valsartan)以摩尔比1:1组成LCZ696.LCZ696是一种血管紧张素受体脑啡肽酶抑制剂.它可降低血压,是治疗心力衰竭的潜在新药.AHU-377是前体药物,可以通过酶裂解乙酯基转换成活性形式LBQ657.据报道,在DAHI-SS大鼠中,AHU-377(30 mg/kg和100 mg/kg,PO)可以剂量依赖的方式引起降压作用.但在DOCA盐高血压大鼠中,降压效果较弱[2,3].
参考文献:
[1] Ksander GM, Ghai RD, deJesus R, Diefenbacher CG, Yuan A, Berry C, Sakane Y, Trapani A. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12; 38(10):1689-700.
[2] Voors AA, Dorhout B, van der Meer P. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.
[3] Laxminarayan G Hegde, Cecile Yu, Cheruvu Madhavi et al. Comparative efficacy of AHU-377, a potent neprilysin inhibitor, in two rat models of volume-dependent hypertension. BMC Pharmacology 2011, 11(Suppl 1):P33.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 430.52 |
Cas No. | 1369773-39-6 |
Formula | C24H28Ca0·5NO5 |
Solubility | ≥17.9 mg/mL in DMSO; ≥2.43 mg/mL in EtOH with gentle warming and ultrasonic; ≥3.3 mg/mL in H2O with gentle warming and ultrasonic |
SDF | Download SDF |
Canonical SMILES | O=C(OCC)[C@@H](C)C[C@@H](NC(CCC([O-])=O)=O)CC1=CC=C(C2=CC=CC=C2)C=C1.[0.5Ca2+] |
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
- 批次:
化学结构
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