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36

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11526	DPP-IV-IN-2 H-Lys(4-nitro-Z)-pyrrolidide	DPP-4	Proteases/Proteasome
	DPP-IV-IN-2 (H-Lys(4-nitro-Z)-pyrrolidide) 是二肽基肽酶 IV 和DP8/9的抑制剂， IC50分别为 0.1 和 0.95 μM。
T10082	DPP-IV-IN-1	Others	Others
	DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).
T1502	Vildagliptin 维达列汀,NVP-LAF 237,维格列汀,LAF237	Apoptosis; Ferroptosis; Proteasome; DPP-4	Apoptosis; Proteases/Proteasome; Ubiquitination
	Vildagliptin (LAF237) 是一种选择性二肽基肽酶IV (DPP-IV) 抑制剂，在人 Caco-2 细胞中抑制 DPP-IV 的IC50为 3.5 nM。它具有出色的口服生物利用度和降血糖活性。
T74978	DPP IV/hCA II-IN-1
	DPP IV/hCA II-IN-1 是一种有效的选择性二肽肽酶 IV (DPP IV) 和碳酸酐酶 (CA) 抑制剂，抑制 DPP IV 的 IC50值为 0.049 μM, 抑制 CA II、CA VB、CA VA、CA IX、CA I 和 CA IV 的 Ki 值分别为 0.0361、0.0428、0.0941、0.1328、0.2615 和 3.034 μM。
T25340	Diprotin A Ile-Pro-Ile,抑二肽素A	DPP-4	Proteases/Proteasome
	Diprotin A (Ile-Pro-Ile) 是二肽基肽酶 IV (DPP-IV) 的抑制剂。
T78410	Gly-Pro-AMC hydrobromide Gly-Pro-AMC HCl
	Gly-Pro-AMC hydrobromide (Gly-Pro-AMC HCl) 为特异性荧光染料，用于细胞荧光检测，检测 Dipeptidyl peptidase IV (DPP-IV) 活性。
T0242L	Sitagliptin phosphate monohydrate MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物	Proteasome; DPP-4; Autophagy	Autophagy; Proteases/Proteasome; Ubiquitination
	Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP-IV 抑制剂，在 Caco-2 细胞提取物中的 IC50 为 19 nM。
T78223	γ-Glu-Tyr gamma-Glutamyltyrosine,gamma-GLU-TYR
	γ-Glu-Tyr (gamma-Glutamyltyrosine) 是一种对二肽基肽酶-IV (DPP-IV) 具有竞争性抑制作用的 kokumi 肽，可用于研究糖尿病。
T68053	Denagliptin GW823093	DPP-4	Proteases/Proteasome
	Denagliptin是一种小分子二肽基肽酶IV（DPP-4）抑制剂，可用于治疗内分泌于代谢疾病，可用于研究2型糖尿病。
T1674	Nateglinide 那格列奈,A4166,Senaglinide	Potassium Channel; Proteasome; PPAR	DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Proteases/Proteasome; Ubiquitination
	Nateglinide (Senaglinide) 是 D-苯丙氨酸的一种衍生物，是口服有效的、短效促胰岛素释放化合物，也是 DPP IV 抑制剂。 Nateglinide 抑制胰岛 β 细胞中 ATP 敏感的 K+通道。Nateglinide 在 2 型糖尿病中具有研究价值。
T26850	BMS-538305 HCl BMS-538305,BMS538305,BMS 538305,BMS-538305 hydrochloride
	BMS-538305 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP-IV).
T11049	Diprotin A TFA Ile-Pro-Pro (TFA)	Others	Others
	Diprotin A (TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
T31378	Denagliptin tosylate GSK-823093,GSK 823093,GW-823093,GW 823093,GSK823093,GW823093
	Denagliptin (GW823093 or GSK-823093) is a dipeptidyl peptidase IV (DPP-IV) inhibitor.
T79911	O-Benzoylhydroxylamine
	O-Benzoyloxyamine 为一种DPP-IV 抑制剂，具备抗糖尿病功能。
T11450	Gosogliptin PF-00734200,PF-734200	Others	Others
	Gosogliptin is a potent and selective dipeptidyl peptidase-IV (DPP-IV) inhibitor.
T63964	DPP-4/GPR119 modulator 2
	DPP-4/GPR119 modulator 2 是二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50: 0.22 μM)，也是一种 GPR119 激动剂 (EC50: 0.95 μM)。DPP-4/GPR119 modulator 2 能够用于研究糖尿病。
T63698	PK44 phosphate
	PK44 phosphate 是二肽基肽酶 IV (DPP-IV) 的有效抑制剂 (IC50: 15.8 nM)。
T74528	DPP-4/GPR119 modulator 1
	DPP-4/GPR119 modulator 1 (Compound 22) 是一种具有口服活性的二肽基肽酶 IV (DPP-IV) 抑制剂和 GPR119激动剂。DPP-4/GPR119 modulator 1 具有降血糖作用，抑制hERG 通道，IC50值为 4.9 µM。DPP-4/GPR119 modulator 1 可用于糖尿病的研究。
T13826	Prodipine hydrochloride	Others	Others
	Prodipine hydrochloride for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit (IC50 of 4.5 μM and 30 μM, respectively).
T21691	NVP DPP 728 dihydrochloride
	NVP-DPP728 是一种有效、可逆、腈依赖性二肽基肽酶 IV (DPP-IV)抑制剂，Ki 值为 11 nM。NVP-DPP728 可抑制胰高血糖素样肽-1 (GLP-1)的降解，从而增强响应于葡萄糖摄入的胰岛素释放。NVP-DPP728 可用于糖尿病研究。
T61414	DPP-4 inhibitor 3
	DPP-4 inhibitor 3 (Compound 5a) 是一种有效的二肽基肽酶 IV (DPP-IV) 抑制剂，IC50为 0.75 nM。DPP-4 inhibitor 3 具有极好的抗氧化和胰岛素性活性。
T26941	Camegliptin RO-4876904-001,R1579,RG1579,RO-4876904,R-1579,RG-1579
	Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.
T82178	H-Pro-Pro-Gln-OH
	H-Pro-Pro-Gln-OH 是一寡肽，表现出对二肽基肽酶 IV (DPP-IV) 的显著抑制作用。
T61076	Vildagliptin dihydrate
	Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1].
T71354	AMG-222 tosylate
	AMG-222 tosylate is a DPP-IV inhibitor in clinical development for type II diabetes.
T27598	Imigliptin Dihydrochloride Imigliptin
	Imigliptin Dihydrochloride, a selective dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type II diabetes.
T68652	Carmegliptin dihydrochloride
	Carmegliptin dihydrochloride is the salt form of Camegliptin (free base), also known as RG-1579 and RO4876904, a dipeptidyl peptidase IV (DPP-4) inhibitor potentially for the treatment of type 2 diabetes.
T39481	NVP-DPP728 dihydrochloride NVP-DPP728 dihydrochloride
	NVP-DPP728 dihydrochloride is a highly potent, selective, and orally active inhibitor of dipeptidyl peptidase IV (DPP-IV), with a binding affinity (K i ) of 11 nM. This compound proves useful for investigating diabetes mellitus in research studies.
T13069	Talabostat isomer mesylate	Others	Others
	Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available inhibitor of dipeptidyl peptidase IV (DPP-IV)(Ki of 0.18 nM).
T22747	DPPI 1c hydrochloride	Others	Others
	DPPI 1c hydrochloride is an inhibitor of dipeptidyl peptidase IV (IC50 = 104 nM) that shows selectivity over enzymes with DPP-like activity (IC50 > 30 μM).
T68863	MK-0626 free base
	MK-0626 is a Dipeptidyl peptidase IV (DPP-4) inhibitor, improving neovascularization by increasing both the number of circulating endothelial progenitor cells and endothelial nitric oxide synthetase expression.
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T30169	ASP-8497 UNII-GC7THT248G,ASP8497,ASP 8497
	ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes.
T73875	Fotagliptin benzoate
	Fotagliptin benzoate，作为一种二肽基肽酶IV (DPP-4) 抑制剂（IC50=2.27 nM），在大鼠和狗中展现了安全性，适用于2型糖尿病的研究。
T68491	Melogliptin
	Melogliptin, also known as EMD-675992 and GRC-8200, is a potent and selective a dipeptidyl peptidase IV (DPP-IV) inhibitor potentially for treatment of type II diabetes. Melogliptin significantly reduced HbA1c from baseline as compared to placebo with a mean average reduction of 0.75 percent in patients receiving 50mg twice daily dose and 0.60 percent in patients receiving 100 mg once daily dose.
T79608	DPP	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	DPP，一种含紫檀芪衍生轴向配体的铂(IV)络合物，能够抑制乳腺癌(BC)细胞的JAK2-STAT3通路并显示出抗增殖特性。它通过激活caspase-3和裂解聚ADP-核糖聚合酶诱导细胞凋亡(apoptosis)，同时促进树突状细胞成熟及抗原呈现功能，并已证明体内具有安全性。

化合物

Cat.No: T11526

Synonym: H-Lys(4-nitro-Z)-pyrrolidide

Target: DPP-4

Cat.No: T10082

Target: Others

Cat.No: T1502

Synonym: 维达列汀,NVP-LAF 237,维格列汀,LAF237

Target: Apoptosis, Ferroptosis, Proteasome, DPP-4

DPP IV/hCA II-IN-1

Cat.No: T74978

Cat.No: T25340

Synonym: Ile-Pro-Ile,抑二肽素A

Target: DPP-4

Gly-Pro-AMC hydrobromide

Cat.No: T78410

Synonym: Gly-Pro-AMC HCl

Sitagliptin phosphate monohydrate

Cat.No: T0242L

Synonym: MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物

Target: Proteasome, DPP-4, Autophagy

Cat.No: T78223

Synonym: gamma-Glutamyltyrosine,gamma-GLU-TYR

Cat.No: T68053

Synonym: GW823093

Target: DPP-4

Cat.No: T1674

Synonym: 那格列奈,A4166,Senaglinide

Target: Potassium Channel, Proteasome, PPAR

Cat.No: T26850

Synonym: BMS-538305,BMS538305,BMS 538305,BMS-538305 hydrochloride

Cat.No: T11049

Synonym: Ile-Pro-Pro (TFA)

Target: Others

Denagliptin tosylate

Cat.No: T31378

Synonym: GSK-823093,GSK 823093,GW-823093,GW 823093,GSK823093,GW823093

O-Benzoylhydroxylamine

Cat.No: T79911

Cat.No: T11450

Synonym: PF-00734200,PF-734200

Target: Others

DPP-4/GPR119 modulator 2

Cat.No: T63964

Cat.No: T63698

DPP-4/GPR119 modulator 1

Cat.No: T74528

Prodipine hydrochloride

Cat.No: T13826

Target: Others

NVP DPP 728 dihydrochloride

Cat.No: T21691

DPP-4 inhibitor 3

Cat.No: T61414

Cat.No: T26941

Synonym: RO-4876904-001,R1579,RG1579,RO-4876904,R-1579,RG-1579

H-Pro-Pro-Gln-OH

Cat.No: T82178

Vildagliptin dihydrate

Cat.No: T61076

AMG-222 tosylate

Cat.No: T71354

Imigliptin Dihydrochloride

Cat.No: T27598

Synonym: Imigliptin

Carmegliptin dihydrochloride

Cat.No: T68652

NVP-DPP728 dihydrochloride

Cat.No: T39481

Synonym: NVP-DPP728 dihydrochloride

Talabostat isomer mesylate

Cat.No: T13069

Target: Others

DPPI 1c hydrochloride

Cat.No: T22747

Target: Others

MK-0626 free base

Cat.No: T68863

Cat.No: T37861

Cat.No: T30169

Synonym: UNII-GC7THT248G,ASP8497,ASP 8497

Fotagliptin benzoate

Cat.No: T73875

Cat.No: T68491

Cat.No: T79608

Target: JAK

Cat. No.	Product Name	Target	Signaling Pathways
TN1418	Azaleatin 杜鹃黄素,2-(3,4-二羟基苯基)-3,7-二羟基-5-甲氧基苯并吡喃-4-酮	DPP-4	Proteases/Proteasome
	Azaleatin 是分离自Rhododendron 种中的 O-甲基化黄酮醇。它是二肽基肽酶-IV 的抑制剂。它在 2 型糖尿病和肥胖症中有研究的价值。
T39219	Ficusonolide
	Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.
T81898	Lyciumamide A
	DPP-IV-IN-5，一种从枸杞果实中分离得到的化合物，对过氧化物酶体增殖物激活受体(PPARγ)展示中等拮抗活性，其EC50值介于10.09至44.26 μM，同时对二肽基肽酶-4 (DPPIV)亦有抑制作用，IC50值为47.13 μM。

天然产物

Cat.No: TN1418

Synonym: 杜鹃黄素,2-(3,4-二羟基苯基)-3,7-二羟基-5-甲氧基苯并吡喃-4-酮

Target: DPP-4

Cat.No: T39219

Cat.No: T81898

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