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32

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T1176 Racecadotril

Acetorphan,消旋卡多曲

Neprilysin; Proteasome Metabolism; Proteases/Proteasome; Ubiquitination
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。
T7693 Thiorphan

Neprilysin Metabolism
Thiorphan 是选择性neprilysin 抑制剂 (IC50:6.9 nM) 。
TQ0106 Sacubitrilat

LBQ-657

Neprilysin Metabolism
Sacubitrilat (LBQ-657) 是活性的脑啡肽酶 (NEP) 抑制剂。
T4574 Sacubitril

AHU 377,AHU377,沙库必曲,AHU-377

Neprilysin Metabolism
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。
T4200 Sacubitril hemicalcium salt

AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt

Neprilysin Metabolism
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。
T2318 Sacubitril/Valsartan

Sacubitril mixture with Valsartan,沙库必曲/缬沙坦,Valsartan,Sacubitril,LCZ696

Apoptosis; RAAS; Neprilysin Apoptosis; Endocrinology/Hormones; Metabolism
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。
T10918 NEP-IN-1

Neprilysin Metabolism
NEP-IN-1 是中性肽链内切酶 (NEP) 的抑制剂 (IC50 = 2 nM)。
T19626 LHW090-A7

(ALPHAS)-3'-氯-ALPHA-[[(1S)-2-乙氧基-1-甲基-2-氧代乙基]氨基][1,1'-联苯]-4-丙酸

Neprilysin Metabolism
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。
T27119L (Rac)-Daglutril

SLV 306 acetic acid,2-((3S)-3-(1-(2-(ethoxycarbonyl)-4-phenylbutyl)cyclopentane-1-carboxamido)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)acetic acid

Others Others
(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。
TP1917L1 Sar-[D-Phe8]-des-Arg9-Bradykinin acetate

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate(126959-88-4 free base)

Bradykinin Receptor GPCR/G Protein
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。
T10671 Candoxatril

UK 79300

Others Others
Candoxatril is an inhibitor neutral endopeptidase (NEP).
T23698 Aladotril

BP1137,BP 1137,BP-1137

Aladotril is an inhibitor of neutral endopeptidase. Its prodrug is aladotrilat.
T12994 SQ28603

Squibb 28603,SQ28,603

Others Others
SQ28603 is a potent and selective neutral endopeptidase 3.4.24.11 (NEP) inhibitor.
T29053 UK-447841

UK 447841

UK-447841, a neutral endopeptidase (NEP) inhibitor, is used potentially for the treatment of female sexual dysfunction.
T28715 Sch 34826

Sch34826,Sch-34826

Sch 34826 is a potent, selective neutral endopeptidase inhibitor.
T70567 CGS 25462

CGS 25462 is a neutral endopeptidase (NEP) inhibitor.
T23699 Aladotrilat

Fasidotrilat

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.
T70471 Cgs 26303

Cgs 26303 is a potent non-peptidic inhibitor of neutral endopeptidase capable of protecting atrial natriuretic peptide from enzymatic degradation.
T31598 Ecadotril

S.049,BAY-y 7432,BAY y 7432,BP 1.02,S049

Ecadotril is a neutral endopeptidase (NEP) inhibitor, which plays an anti hypertensive role.
T70698 MDL-100173

MDL-100173 is a dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitor.
T26048 RB 101

RB101,RB-101

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.
T30701 Candoxatrilat

UK69578,UK 69578,U 73967,U-73967,U73967,UK-69578

Candoxatrilat (U 73967, UK69578) is an active neutral endopeptidase inhibitor that reduces atrial natriuretic peptide degradation.
T29052 UK-414,495

UK 414495,UK414,495,UK414495,UK-414495

UK-414,495 is a potent, selective inhibitor of the neutral endopeptidase, the enzyme normally serves to break down the neuropeptide VIP.
T15696 NEP-IN-2

Others Others
NEP-IN-2 is an inhibitor of neutral endopeptidase. It also is used in the research of proliferation in atherosclerosis, restenosis.
T68601 Azidothiorphan

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.
T16840 Sampatrilat

UK-81252

Others Others
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).
T37890 GLP-1(28-36)amide

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].
TP1917 Sar-[D-Phe8]-des-Arg9-Bradykinin

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.
T61095 SCH-42354

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].
T36943 Aminopeptidase N Inhibitor

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.
T81444 PL-3994

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。
T76191 GLP-1(28-36)amide TFA

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。

化合物

Racecadotril
Cat.No: T1176
Synonym: Acetorphan,消旋卡多曲
Target: Neprilysin, Proteasome
Thiorphan
Cat.No: T7693
Synonym:
Target: Neprilysin
Sacubitrilat
Cat.No: TQ0106
Synonym: LBQ-657
Target: Neprilysin
Sacubitril
Cat.No: T4574
Synonym: AHU 377,AHU377,沙库必曲,AHU-377
Target: Neprilysin
Sacubitril hemicalcium salt
Cat.No: T4200
Synonym: AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt
Target: Neprilysin
Sacubitril/Valsartan
Cat.No: T2318
Synonym: Sacubitril mixture with Valsartan,沙库必曲/缬沙坦,Valsartan,Sacubitril,LCZ696
Target: Apoptosis, RAAS, Neprilysin
NEP-IN-1
Cat.No: T10918
Synonym:
Target: Neprilysin
LHW090-A7
Cat.No: T19626
Synonym: (ALPHAS)-3'-氯-ALPHA-[[(1S)-2-乙氧基-1-甲基-2-氧代乙基]氨基][1,1'-联苯]-4-丙酸
Target: Neprilysin
(Rac)-Daglutril
Cat.No: T27119L
Synonym: SLV 306 acetic acid,2-((3S)-3-(1-(2-(ethoxycarbonyl)-4-phenylbutyl)cyclopentane-1-carboxamido)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)acetic acid
Target: Others
Sar-[D-Phe8]-des-Arg9-Bradykinin acetate
Cat.No: TP1917L1
Synonym: Sar-[D-Phe8]-des-Arg9-Bradykinin acetate(126959-88-4 free base)
Target: Bradykinin Receptor
Candoxatril
Cat.No: T10671
Synonym: UK 79300
Target: Others
Aladotril
Cat.No: T23698
Synonym: BP1137,BP 1137,BP-1137
Target:
SQ28603
Cat.No: T12994
Synonym: Squibb 28603,SQ28,603
Target: Others
UK-447841
Cat.No: T29053
Synonym: UK 447841
Target:
Sch 34826
Cat.No: T28715
Synonym: Sch34826,Sch-34826
Target:
CGS 25462
Cat.No: T70567
Synonym:
Target:
Aladotrilat
Cat.No: T23699
Synonym: Fasidotrilat
Target:
Cgs 26303
Cat.No: T70471
Synonym:
Target:
Ecadotril
Cat.No: T31598
Synonym: S.049,BAY-y 7432,BAY y 7432,BP 1.02,S049
Target:
MDL-100173
Cat.No: T70698
Synonym:
Target:
RB 101
Cat.No: T26048
Synonym: RB101,RB-101
Target:
Candoxatrilat
Cat.No: T30701
Synonym: UK69578,UK 69578,U 73967,U-73967,U73967,UK-69578
Target:
UK-414,495
Cat.No: T29052
Synonym: UK 414495,UK414,495,UK414495,UK-414495
Target:
NEP-IN-2
Cat.No: T15696
Synonym:
Target: Others
Azidothiorphan
Cat.No: T68601
Synonym:
Target:
Sampatrilat
Cat.No: T16840
Synonym: UK-81252
Target: Others
GLP-1(28-36)amide
Cat.No: T37890
Synonym:
Target:
Sar-[D-Phe8]-des-Arg9-Bradykinin
Cat.No: TP1917
Synonym:
Target:
SCH-42354
Cat.No: T61095
Synonym:
Target:
Aminopeptidase N Inhibitor
Cat.No: T36943
Synonym:
Target:
PL-3994
Cat.No: T81444
Synonym:
Target:
GLP-1(28-36)amide TFA
Cat.No: T76191
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6627 Phosphoramidon Disodium

Phosphoramidon Disodium Salt,磷酰胺二钠

RAAS; Neprilysin; Others Endocrinology/Hormones; Metabolism; Others
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。
T1168 Desonide

Tridesilon,地索奈德,Locapred,Prednacinolone

Glucocorticoid Receptor Endocrinology/Hormones
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。

天然产物

Phosphoramidon Disodium
Cat.No: T6627
Synonym: Phosphoramidon Disodium Salt,磷酰胺二钠
Target: RAAS, Neprilysin, Others
Desonide
Cat.No: T1168
Synonym: Tridesilon,地索奈德,Locapred,Prednacinolone
Target: Glucocorticoid Receptor
TargetMol Loading
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