DPP-4-IN-1

DPP-4-IN-1 (compound d1) is a highly potent inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC 50 of 49 nM, making it suitable for diabetes research [1]. It shares structural similarities to Alogliptin and can be effectively utilized for studying diabetes-related mechanisms.

DPP-4-IN-16 (Compound 92) 是一种高效的二肽基肽酶-4 (DPP-4) 抑制剂 (IC50=0.8 nM)。它通过抑制DPP-4对GLP-1和GIP等肠促胰岛素的降解，促进胰岛素分泌并控制血糖水平。DPP-4-IN-16 有可能用于2型糖尿病的研究。

DPP-4-IN-10 (compound 1) 是DPP-4抑制剂，具备口服活性。它能有效阻止GLP-1和GIP的降解，从而有助于控制2型糖尿病 (T2MD) 的血糖水平。

DPP-4-IN-12 (compound 46) 作为一种高效的DPP-4抑制剂，其IC50仅为2 nM，主要应用于2型糖尿病的研究领域。

DPP-4-IN-13 (compound 9i) 作为竞争性DPP4抑制剂，展现出9.25 μM的IC50，适于2型糖尿病研究应用。

DPP-4-IN-14（compound 30）为DPP-4抑制剂，IC50值为12.82 nM。

DPP-4-IN-15 (Compound 22) 是一种非竞争性抑制剂，针对二肽基肽酶-4 (DPP-4)，IC50值为8.24 μM。

DPP-4-IN-17 是一种口服活性的选择性二肽基肽酶-4 (DPP-4) 抑制剂，其IC50值为0.12 nM。DPP-4-IN-17 增加酶的Km值（75.73 μM 对比底物单独的27.18 μM），并降低催化效率。在Streptozotocin(STZ)/Nicotinamide(NA) 诱导的糖尿病大鼠模型中，DPP-4-IN-17 可以降低血糖水平并逆转体重减轻。DPP-4-IN-17 可用于2型糖尿病 (T2DM) 的研究。

DPP-4-IN-11 (compound 10) 为一种抗2型糖尿病活性的口服DPP-4抑制剂,其IC50值为2.75 μM.该化合物通过抑制α-葡萄糖苷酶(IC50=3.02 μM)和α-淀粉酶(IC50=3.3 μM)来降低血糖.

Sitagliptin (MK0431) 是一种有效的 DPP4抑制剂，在 Caco-2 细胞中，IC50值为 19 nM。它是一种新型口服降糖药，可单独使用或与二甲双胍或噻唑烷二酮联合用于治疗 2 型糖尿病。

Teneligliptin hydrobromide (MP-513(hydrobromide)) 是β2肾上腺素能受体 (β2AR) 阻滞剂，具有抗高血压、抗氧化、清除自由基的活性。

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。

YH18968, 作为GPR119激动剂, 有助于提高葡萄糖耐受性，并增强降低血糖的效果。在与二肽基肽酶4 (DPP-4) 抑制剂联合治疗时，YH18968能够提升正常小鼠中活性GLP-1的血浆水平。

Cetagliptin 是一种口服有效的二肽基肽酶 4 (dipeptidyl peptidase 4，DPP-4) 和 CYP2D6 抑制剂（IC50 为 6 µM），同时也是 P-糖蛋白 (P-glycoprotein) 的底物。Cetagliptin 通过减少 GLP-1 的降解作用维持餐后血糖水平，被用于 2 型糖尿病的研究。

(2S,4R)-Teneligliptin 是一种二肽基肽酶 IV (DPP-4) 的特异性抑制剂，通过提高血浆中活性胰高血糖素样肽-1 (GLP-1) 浓度，在血糖升高时增强胰岛素的分泌，从而实现降血糖效果。此化合物有潜力用于2型糖尿病的相关研究。

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

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.

Teneligliptin hydrobromide hydrate 是一种有效的 DPP-4抑制剂，可在体外竞争性抑制人血浆、大鼠血浆和重组人 DPP-4 ，IC50值约为 1 nM。

DPP-4-IN-2 (compound b2) 是 Alogliptin 的结构类似物，可以用于研究糖尿病。DPP-4-IN-2 是二肽基肽酶 4 (DPP-4)的有效抑制剂，IC50值为 79 nM。

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。

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。

Sitagliptin fenilalanil hydrochloride 是一种二肽氨基肽酶 (DPP-4) 抑制剂。

Albiglutide fragment (GLP-1 (7-36) analog) TFA为Albiglutide活性片段，代表胰高血糖素样肽-1(GLP-1)模拟物，属长效GLP-1受体激动剂。由GLP-1二聚体抗DPP-4特性与人白蛋白基因融合而成，本化合物在降低糖化血红蛋白(A1C)方面表现显著，主要应用于2型糖尿病(T2D)的相关研究。

DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂，具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性，并剂量依赖性地降低 TNF-α、IL-6 和 IL-1β 的表达水平[1]。