dpp iv

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。

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。

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。

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。

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。

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.

Vildagliptin-d7 是 Vildagliptin 的氘代化合物。Vildagliptin 的 CAS 号为 274901-16-5。Vildagliptin 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。

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

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.

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。

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.

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).

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。

AMG-222 tosylate is a DPP-IV inhibitor in clinical development for type II diabetes.

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。

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。

VAMP 是一种四肽和竞争性二肽基肽酶 IV (DPP-IV) 抑制剂，其 IC50 为 1.00 μM，Kd 为 6.89 μM。VAMP 有效靶向 DPP-IV-GLP-1 轴，适用于 2 型糖尿病的研究。

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。

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.

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.