neutral endopeptidase

NEP-IN-1 是中性肽链内切酶 (NEP) 的抑制剂 (IC50 = 2 nM)。

Racecadotril (Acetorphan) 是一种中性内肽酶 (NEP) 抑制剂，具有止泻作用。Racecadotril 及其活性代谢物 Thiorphan 抑制小鼠脑中纯化的NEP 活性，Ki 分别为 4500 和 6.1 nM。

Sacubitril Valsartan (LCZ696)，以1:1摩尔比由Valsartan（一种ARB）和Sacubitril（AHU377）组成，为创新口服血管紧张素受体-脑啡肽酶（ARN）双重抑制剂，旨在治疗高血压与心力衰竭。其作用机制包括抑制炎症、氧化应激及细胞凋亡，有助于改善糖尿病心肌病。

Sacubitril (AHU-377) 是一种有效的NEP 抑制剂，IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。

Sacubitril hemicalcium salt (AHU377 calcium salt) 是一种有效的 NEP 抑制剂，IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。

Desonide (Prednacinolone) 是一种非氟化皮质类固醇抗炎剂，能够作用于糖皮质激素受体。

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate(126959-88-4 free base) 是一种有效的选择性缓激肽 B1 受体激动剂（兔主动脉中的 EC50 = 9.02 nM），对氨肽酶、激肽酶 I 和 II (ACE) 以及中性内肽酶切割具有抗性。在体内表现出降血压和血管生成活性。

(Rac)-Daglutril (SLV 306 acetic acid) 是 Daglutril 的消旋体。Daglutril 是一种口服活性的混合中性内肽酶 内皮素转化酶抑制剂，正在开发用于治疗原发性高血压和充血性心力衰竭。

LHW090-A7 是一种中性肽链内切酶 (NEP) 抑制剂，是一种负责脑啡肽代谢失活的酶。

Thiorphan 是选择性neprilysin 抑制剂 (IC50:6.9 nM) 。

Sacubitrilat (LBQ-657) 是活性的脑啡肽酶 (NEP) 抑制剂。

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

Candoxatrilat (U 73967, UK69578) is an active neutral endopeptidase inhibitor that reduces atrial natriuretic peptide degradation.

MDL-100173 is a dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitor.

Azidothiorphan is a photoaffinity ligand for the active site of the neutral endopeptidase 24.11. After ultraviolet irradiation the inhibitor binds irreversibly to the enzyme, and photolabeling occurs at the active site. The competitive inhibitor thiorphan protects the endopeptidase from inactivation.

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

Potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

GLP-1(28-36)amide TFA，为GLP-1 C-端九肽段，主要通过中性内肽酶（NEP）裂解GLP-1生成。该化合物作为一种抗氧化剂，能靶向线粒体，抑制线粒体通透性转变（MPT），显示出抗糖尿病和心脏保护的功效。

Ecadotril is a neutral endopeptidase (NEP) inhibitor, which plays an anti hypertensive role.

NEP-IN-2 is an inhibitor of neutral endopeptidase. It also is used in the research of proliferation in atherosclerosis, restenosis.

Sampatrilat is an effecive and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase. Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM).

Phosphoramidon Disodium (Phosphoramidon Disodium Salt) Salt 是一种金属蛋白酶 (metalloprotease) 抑制剂 。Phosphoramidon Disodium Salt 抑制内皮素转化酶 (ECE) ，中性肽内切酶 (NEP) 和血管紧张素转换酶 (ACE) 的IC50分别为 3.5 ，0.034 和 78 μM。

PL-3994作为NPR-A的激动剂，展现了对中性肽酶的耐药特性，具有支气管扩张效应。对预收缩豚鼠气管，PL-3994表现出浓度依赖性的弛豫作用，其IC50值为42.7 nM。

GLP-1(28-36)amide, a C-terminal nonapeptide derived from the cleavage of GLP-1 by neutral endopeptidase (NEP), is a significant product. It functions as an antioxidant and primarily targets the mitochondrion, where it effectively inhibits mitochondrial permeability transition (MPT). This compound exhibits anti-diabetic properties and demonstrates cardioprotection effects[1].

SQ28603 is a potent and selective neutral endopeptidase 3.4.24.11 (NEP) inhibitor.

Aladotril is an inhibitor of neutral endopeptidase. Its prodrug is aladotrilat.

UK-447841, a neutral endopeptidase (NEP) inhibitor, is used potentially for the treatment of female sexual dysfunction.

CGS 25462 is a neutral endopeptidase (NEP) inhibitor.

UK-414,495 is a potent, selective inhibitor of the neutral endopeptidase, the enzyme normally serves to break down the neuropeptide VIP.

Sch 34826 is a potent, selective neutral endopeptidase inhibitor.

SCH-42354 is a potent, orally active inhibitor of neutral endopeptidase (NEP), serving as the active form of the prodrug SCH-42495. By inhibiting NEP hydrolysis, SCH-42354 enhances the activity of atrial natriuretic peptide (ANP) and prevents the hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. Furthermore, SCH-42354 exhibits antihypertensive activity [1] [2].

Cgs 26303 is a potent non-peptidic inhibitor of neutral endopeptidase capable of protecting atrial natriuretic peptide from enzymatic degradation.