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My CartCAS：936623-90-4
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to yellow Solid
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| CAS | 936623-90-4 |
| Name | Entresto |
| Molecular Formula | C24H29N5O3·C24H29NO5·5/2H2O·3Na |
| Molecular Weight | 961.02 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 000-000-0 |
| MDL | MFCD28900676 |
| SMILES | O=C(CCC([O-])=O)N([C@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@@H](C)C(OCC)=O)[H].[O-]C([C@@H](N(C(CCCC)=O)CC3=CC=C(C4=CC=CC=C4C5=NN=N[N-]5)C=C3)C(C)C)=O.[Na+].[Na+].[Na+].[2.5H2O] |
| Target Point | Angiotensin Receptor；RAAS |
| Passage | GPCR & G Protein |
| Background | It is a dual inhibitor of angiotensin II receptor and enkephalinase. |
| Biological Activity | Entresto是血管紧张素II受体和脑啡肽酶的双抑制剂。[1-3] |
| In Vivo | Entresto发挥降血压作用。 Entresto的血压降低与尿钠排泄和交感神经活动抑制的显著增加有关。与缬沙坦相比，Entresto显著改善高盐负荷SHRcp的心脏肥大和炎症，冠状动脉重塑和血管内皮功能障碍[1]。 Entresto的脑啡肽酶抑制剂成分LBQ657抑制肥大但不抑制纤维化。 Entresto的血管紧张素受体阻滞剂成分，缬沙坦抑制肥大和纤维化。双缬沙坦+ LBQ增强缬沙坦的抑制作用，最高剂量完全消除血管紧张素II介导的作用[2]。 Entresto预处理可减少缺血区域。通过用Entresto预处理，缺血区域周围区域的脑血流减少显著减弱。 Entresto预处理显著降低了缺血侧皮质中超氧阴离子产生的增加[3]。 |
| Animal Experiment | 大鼠：Entresto或缬沙坦在黑暗期开始时每天一次以明胶迷你胶囊中的粉末形式口服给药。给予载体组大鼠空胶囊。微型遥测设备植入12或13周龄的SHR中。在黑暗和光照期间监测BP和心率变异性，收缩压的低频功率和自发的压力感受器反射增益。 SHR在16周龄时分为3组：(i)载体，(ii)Entresto，和(iii)缬沙坦。 Entresto和缬沙坦的剂量分别为16至18周龄的20和10mg/kg /天，以及18至23周龄的60和30mg/kg /天。在21周龄时，SHR饮食从高盐饮食转为低盐饮食[1]。小鼠：在MCA闭塞前，每天用VAL(每天3mg/kg)或Entresto(每天6mg/kg)口服胶囊作为粉末在明胶迷你胶囊中处理2周。在VAL或Entresto预处理2周后测量体重。收缩压，舒张压和心率在10周龄时通过遥测测量[3]。 |
| Data Literature Source | [1]. Huo H，et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605. [2]. von Lueder TG，et al. Angiotensin receptor neprilysin inhibitor Entresto attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8. [3]. Bai HY，et al. Pre-treatment with Entresto，an orally active angiotensin receptor neprilysin inhibitor，prevents ischemic brain damage. Eur J Pharmacol. 2015 Sep 5;762:293-8. |
| Unit | Bottle |
| Specification | 5mg 10mg 25mg |
是血管紧张素II受体和脑啡肽酶的双抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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