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68

抑制剂 & 化合物

9

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Cat. No. Product Name Target Signaling Pathways
T12546 Prolyl Endopeptidase Inhibitor 1

(Boc)-Prolyl-prolinal,BPP,Boc-Pro-prolinal

Others Others
Prolyl Endopeptidase Inhibitor 1 is a potent inhibitor of prolyl endopeptidase (PEP; PE)(Ki : 15 nM) , has anti-amnesic effect.
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。
T8657 KYP-2047

Others Others
KYP-2047 是一种非常有效的选择性脯氨酰寡肽酶 (POP) 抑制剂。
T9713 δ-secretase inhibitor 11

Beta Amyloid; Caspase Apoptosis; Neuroscience; Proteases/Proteasome
δ-secretase inhibitor 11是一种分泌酶抑制剂,可用作 阿尔茨海默病(AD) 治疗转化开发的先导化合物。
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。
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。
T9855 BR102910 

4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-

Others Others
BR102910 (4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-) 是一种选择性的成纤维细胞活化蛋白(FAP)的抑制剂。
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。
T10671 Candoxatril

UK 79300

Others Others
Candoxatril is an inhibitor neutral endopeptidase (NEP).
T41032 Lysostaphin

Antibacterial Microbiology/Virology
Lysostaphin是一种具有强大抗葡萄球菌活性的化合物,通过三种不同的酶展现其酶促活性:glycylglycine endopeptidase、endo-β-N-acetyl glucosamidase和N-acetyl muramyl-L-alanine amidase。
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)。
T27730 KGP94

KGP-94,KGP 94

Cysteine Protease Proteases/Proteasome
KGP94 是一种有效的、选择性的和竞争性的溶酶体内肽酶抑制剂。
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。
T35233 Y-29794 Tosylate

Y 29794,Y29794 tosylate,Y29794,Y-29794

Prolyl Endopeptidase (PREP) Metabolism; Proteases/Proteasome
Y-29794 Tosylate (Y-29794) 是一种具有口服活性、有效且特异性的非肽脯氨酰内肽酶 (PPCE) 抑制剂。
T12770 RR-11a analog

aza-peptide Michael acceptor, 7a

Parasite Microbiology/Virology
RR-11a analog (aza-peptide Michael acceptor, 7a) 是一种天冬酰胺酰内肽酶抑制剂,对阴道毛滴虫中的 AE1、蓖麻硬蜱中的 AE 和曼氏血吸虫中的 AE 的 IC50 分别为 4.5 nM、4.5 nM 和 31 nM。
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。
T27716 KC-12615

KC12615

KC-12615 is an inhibitior of endopeptidase.
T26659 ARI-3531

ARI 3531

ARI-3531 is a selective prolyl endopeptidase inhibitor.
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.
T23541 Y-29794 oxalate

Others Others
Inhibitor of prolyl endopeptidase
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.
T27989 MDK0734

Cathepsin B Inhinitor-42

MDK0734 is a selective inhibitor of cathepsin B endopeptidase and exopeptidase activities.
T25973 Poststatin

Poststatin is a prolyl endopeptidase inhibitor produced by Streptomyces viridochromogenes MH534-30F3.
T70471 Cgs 26303

Cgs 26303 is a potent non-peptidic inhibitor of neutral endopeptidase capable of protecting atrial natriuretic peptide from enzymatic degradation.
T70567 CGS 25462

CGS 25462 is a neutral endopeptidase (NEP) inhibitor.
T17279 Z-321

Others Others
Z-321 is an inhibitor of prolyl endopeptidase.
T28246 ONO-1603

ONO1603

ONO-1603, a prolyl endopeptidase inhibitor, is used potentially for the treatment of Alzheimer's disease.
T23699 Aladotrilat

Fasidotrilat

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.
T28003 MDK7677

Cathepsin B Inhinitor-17,MDK 7677

MDK7677 is a selective inhibitor of cathepsin B endopeptidase and exopeptidase activities.
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.
TP1900 Hemopressin (human, mouse)

Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinoc
T70698 MDL-100173

MDL-100173 is a dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitor.
T25955 Picromycin

Antibiotic B 62169A,Amaromycin,Albomycetin,Pikromycin

Picromycin is a 14-membered macrolide antibiotic and Prolyl endopeptidase (PREP) inhibitor. Pikromycin shows activity against gram-positive bacteria including mycobacteria.
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.
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.
T25890 NSC-84096

CID 256758,CID-256758,CID256758

NSC-84096 is an endopeptidase activity inhibitor of botulinum neurotoxin type A light chain (rBoNT/A-LC).
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.
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.
TP1210 Bradykinin (1-7)

Bradykinin Fragment 1-​7

Bradykinin (1-7), an amino-truncated peptide derived from Bradykinin, is a metabolite formed through enzymatic cleavage by endopeptidase.
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.
T74674 Z-Thioprolyl-Thiazolidine

Z-Thioprolyl-Thiazolidine 是一种有效且特异的脯氨酰内肽酶 (prolyl endopeptidase) 抑制剂,对牛脑的脯氨酰内肽酶 Ki 为 0.36 nM。
T78363 Aspergillopepsin I

Aspergillus acid protease

Aspergillopepsin I (Aspergillus acid protease) 是一种属于天冬氨酸内肽酶类,能广泛特异性催化水解蛋白质中的肽键。
T38116 Fmoc-Ala-Glu-Asn-Lys-NH2

Fmoc-Ala-Glu-Asn-Lys-NH2

Fmoc-Ala-Glu-Asn-Lys-NH2 is a peptide inhibitor that selectively targets asparagine endopeptidase (AEP) and inhibits the cleavage of amyloid precursor protein (APP). AEP, a pH-controlled cysteine proteinase, plays a crucial role in the proteolytic processing of APP, and its activity is enhanced during the aging process [1].
T70878 P516-0475

P516-0475 is a novel chemical inducer of Streptococcus quorum sensing acts by inhibiting the pheromone-degrading endopeptidase PepO. This compound induces quorum sensing by stabilizing SHP pheromones in culture.
TP1901 Hemopressin(rat)

Hemopressin (rat)

Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinoc

化合物

Prolyl Endopeptidase Inhibitor 1
Cat.No: T12546
Synonym: (Boc)-Prolyl-prolinal,BPP,Boc-Pro-prolinal
Target: Others
Thiorphan
Cat.No: T7693
Synonym:
Target: Neprilysin
Sacubitrilat
Cat.No: TQ0106
Synonym: LBQ-657
Target: Neprilysin
KYP-2047
Cat.No: T8657
Synonym:
Target: Others
δ-secretase inhibitor 11
Cat.No: T9713
Synonym:
Target: Beta Amyloid, Caspase
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
Racecadotril
Cat.No: T1176
Synonym: Acetorphan,消旋卡多曲
Target: Neprilysin, Proteasome
BR102910 
Cat.No: T9855
Synonym: 4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-
Target: Others
Sacubitril/Valsartan
Cat.No: T2318
Synonym: Sacubitril mixture with Valsartan,沙库必曲/缬沙坦,Valsartan,Sacubitril,LCZ696
Target: Apoptosis, RAAS, Neprilysin
Candoxatril
Cat.No: T10671
Synonym: UK 79300
Target: Others
Lysostaphin
Cat.No: T41032
Synonym:
Target: Antibacterial
NEP-IN-1
Cat.No: T10918
Synonym:
Target: Neprilysin
KGP94
Cat.No: T27730
Synonym: KGP-94,KGP 94
Target: Cysteine Protease
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
Y-29794 Tosylate
Cat.No: T35233
Synonym: Y 29794,Y29794 tosylate,Y29794,Y-29794
Target: Prolyl Endopeptidase (PREP)
RR-11a analog
Cat.No: T12770
Synonym: aza-peptide Michael acceptor, 7a
Target: Parasite
(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
KC-12615
Cat.No: T27716
Synonym: KC12615
Target:
ARI-3531
Cat.No: T26659
Synonym: ARI 3531
Target:
Aladotril
Cat.No: T23698
Synonym: BP1137,BP 1137,BP-1137
Target:
SQ28603
Cat.No: T12994
Synonym: Squibb 28603,SQ28,603
Target: Others
Y-29794 oxalate
Cat.No: T23541
Synonym:
Target: Others
UK-447841
Cat.No: T29053
Synonym: UK 447841
Target:
Sch 34826
Cat.No: T28715
Synonym: Sch34826,Sch-34826
Target:
MDK0734
Cat.No: T27989
Synonym: Cathepsin B Inhinitor-42
Target:
Poststatin
Cat.No: T25973
Synonym:
Target:
Cgs 26303
Cat.No: T70471
Synonym:
Target:
CGS 25462
Cat.No: T70567
Synonym:
Target:
Z-321
Cat.No: T17279
Synonym:
Target: Others
ONO-1603
Cat.No: T28246
Synonym: ONO1603
Target:
Aladotrilat
Cat.No: T23699
Synonym: Fasidotrilat
Target:
MDK7677
Cat.No: T28003
Synonym: Cathepsin B Inhinitor-17,MDK 7677
Target:
Ecadotril
Cat.No: T31598
Synonym: S.049,BAY-y 7432,BAY y 7432,BP 1.02,S049
Target:
Hemopressin (human, mouse)
Cat.No: TP1900
Synonym:
Target:
MDL-100173
Cat.No: T70698
Synonym:
Target:
Picromycin
Cat.No: T25955
Synonym: Antibiotic B 62169A,Amaromycin,Albomycetin,Pikromycin
Target:
Azidothiorphan
Cat.No: T68601
Synonym:
Target:
RB 101
Cat.No: T26048
Synonym: RB101,RB-101
Target:
NSC-84096
Cat.No: T25890
Synonym: CID 256758,CID-256758,CID256758
Target:
UK-414,495
Cat.No: T29052
Synonym: UK 414495,UK414,495,UK414495,UK-414495
Target:
Candoxatrilat
Cat.No: T30701
Synonym: UK69578,UK 69578,U 73967,U-73967,U73967,UK-69578
Target:
Bradykinin (1-7)
Cat.No: TP1210
Synonym: Bradykinin Fragment 1-​7
Target:
NEP-IN-2
Cat.No: T15696
Synonym:
Target: Others
Z-Thioprolyl-Thiazolidine
Cat.No: T74674
Synonym:
Target:
Aspergillopepsin I
Cat.No: T78363
Synonym: Aspergillus acid protease
Target:
Fmoc-Ala-Glu-Asn-Lys-NH2
Cat.No: T38116
Synonym: Fmoc-Ala-Glu-Asn-Lys-NH2
Target:
P516-0475
Cat.No: T70878
Synonym:
Target:
Hemopressin(rat)
Cat.No: TP1901
Synonym: Hemopressin (rat)
Target:
Cat. No. Product Name Target Signaling Pathways
TN4442 Linderene acetate

Prolyl Endopeptidase (PREP) Metabolism; Proteases/Proteasome
Linderene acetate 是一种脯氨酸肽链内切酶抑制剂,分离自Lindera strychnifolia 中。
T2717 Salidroside

红景天苷,Rhodioloside

Apoptosis; mTOR Apoptosis; PI3K/Akt/mTOR signaling
Salidroside (Rhodioloside) 是一种从红景天中分离出来的具有生物活性的酚苷化合物,是一种脯氨酰内肽酶抑制剂。它能通过激活 mTOR 信号缓解肿瘤恶病质小鼠模型中的恶病质症状,还能通过增强 PINK1/Parkin 介导的线粒体自噬来保护多巴胺能神经元。
T2S0618 β-Elemonic Acid

3-oxo Tirucallic Acid,β-岚香酮酸,Beta-Elemonic acid,3-Oxotirucallenoic Acid,β-榄香酮酸,Elemadienonic Acid

Apoptosis; Reactive Oxygen Species; COX Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
β-Elemonic Acid (3-Oxotirucallenoic Acid) 是从乳香树中分离得到的一种三萜,具有抗癌和抗炎作用。它抑制脯氨酰内肽酶,诱导细胞凋亡,活性氧和COX-2表达。
T3891 Oroxylin A-7-O-glucuronide

Oroxylin A Glucoronide,千层纸素A-7-0-Β-D-葡萄糖醛酸苷,Oroxyloside,Oroxylin A 7-O-beta-D-glucuronide

Others Others
Oroxylin A-7-O-glucuronide (Oroxylin A Glucoronide) 是一种类黄酮葡糖苷酸,提取自 Scutellaria baicalensis 干燥的根中,具有脯氨酰寡肽酶(POP)抑制作用。
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。
T2775 Baicalin

黄芩苷,黄岑苷,Baicalein 7-O-β-D-glucuronide

NF-κB; HIV Protease; GABA Receptor; Autophagy Autophagy; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome
Baicalin (Baicalein 7-O-β-D-glucuronide) 是一种从黄芩中分离出来的脯氨酰内肽酶抑制剂,具有抗氧化、抗肿瘤、抗 HIV 的特性。
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。
TN4917 Rosenonolactone

Others Others
Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin.
T20541 Phosphoramidon

Phosphoramidon is a membrane metallo-endopeptidase & endothelin-converting enzyme inhibitor and thermolysin inhibitor, which is obtained from culture filtrate of Streptomyces tanashiensis.

天然产物

Linderene acetate
Cat.No: TN4442
Synonym:
Target: Prolyl Endopeptidase (PREP)
Salidroside
Cat.No: T2717
Synonym: 红景天苷,Rhodioloside
Target: Apoptosis, mTOR
β-Elemonic Acid
Cat.No: T2S0618
Synonym: 3-oxo Tirucallic Acid,β-岚香酮酸,Beta-Elemonic acid,3-Oxotirucallenoic Acid,β-榄香酮酸,Elemadienonic Acid
Target: Apoptosis, Reactive Oxygen Species, COX
Oroxylin A-7-O-glucuronide
Cat.No: T3891
Synonym: Oroxylin A Glucoronide,千层纸素A-7-0-Β-D-葡萄糖醛酸苷,Oroxyloside,Oroxylin A 7-O-beta-D-glucuronide
Target: Others
Phosphoramidon Disodium
Cat.No: T6627
Synonym: Phosphoramidon Disodium Salt,磷酰胺二钠
Target: RAAS, Neprilysin, Others
Baicalin
Cat.No: T2775
Synonym: 黄芩苷,黄岑苷,Baicalein 7-O-β-D-glucuronide
Target: NF-κB, HIV Protease, GABA Receptor, Autophagy
Desonide
Cat.No: T1168
Synonym: Tridesilon,地索奈德,Locapred,Prednacinolone
Target: Glucocorticoid Receptor
Rosenonolactone
Cat.No: TN4917
Synonym:
Target: Others
Phosphoramidon
Cat.No: T20541
Synonym:
Target:
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