dpp-iv

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。

Gosogliptin（戈格列汀）是一种有效的口服活性、高度选择性和竞争性的DPP-4（二肽基肽酶4）抑制剂，提高肠促胰岛素肽(GLP-1)和葡萄糖依赖性促胰岛素多肽（GIP）的水平，从而增强胰岛素分泌并降低血糖水平。在动物实验中，Gosogliptin能够快速可逆地抑制血浆DPP-4活性。

Saikogenin A 是一种二肽基肽酶 IV 抑制剂，可从中药柴胡中提取。

Dipeptidyl peptidaseIV (DPP-IV) 是一种具有多重生物功能的蛋白酶,不仅能促使诸如胰高血糖素样肽 1 (GLP-1) 和葡萄糖依赖性胰岛素样多肽 (GIP) 等肠促胰岛素激素失活,还能作为多种细胞外分子的结合蛋白和配体.此外,Dipeptidyl peptidaseIV 在糖尿病和肿瘤领域的研究中也显示出其重要应用价值.

DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).

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。

Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.

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。

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。

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。

MK-0626是一种可口服的二肽基肽酶IV（DPP-4）抑制剂，通过增强AMPK活性，减轻肝脏脂肪变性和蓄积。MK-0626通过恢复GLP-1R的表达减轻了TAC诱导的糖尿病胰岛损伤。MK-0626能够通过增加循环内皮祖细胞的数量和内皮型一氧化氮合酶的表达，促进新血管生成。

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, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Diprotin A (TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).

Talabostat isomer mesylate, an isomer of talabostat mesylate, is a potent, nonselective, and orally available inhibitor of dipeptidyl peptidase IV (DPP-IV) with a Ki of 0.18 nM. Talabostat (PT100, Val-boroPro) is notable for its efficacy in inhibiting DPP-IV.

Prodipine hydrochloride for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit (IC50 of 4.5 μM and 30 μM, respectively).

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。

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).

Diprotin A (Ile-Pro-Ile) 是二肽基肽酶 IV (DPP-IV) 的抑制剂。

BMS-538305 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP-IV).

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.

Denagliptin (GW823093 or GSK-823093) is a dipeptidyl peptidase IV (DPP-IV) inhibitor.

Teneligliptin (MP-513) 是一种用于治疗 2 型糖尿病的新型二肽基肽酶 4 （DPP IV） 抑制剂，具有降糖活性，可用于研究肥胖和糖尿病。

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.

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.