dipeptidyl peptidase 1

Brensocatib (AZD7986) 是一种二肽基肽酶 1 (DPP1) 抑制剂，在人，小鼠，大鼠，狗和兔中的pIC50分别为 6.85, 7.6, 7.7, 7.8 和 7.8。

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

Saxagliptin hydrate (Onglyza hydrate) 是一种选择性，竞争性，可逆性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin hydrate 能够用于 2 型糖尿病的研究。

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。

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.

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。

Retagliptin Phosphate (SP 2086) 是一种选择性、竞争性、口服活性的二肽基肽酶 4 (DPP-4) 抑制剂。Retagliptin phosphate 能够用于 2 型糖尿病 (T2DM) 的研究。

Puromycin aminonucleoside（NSC 3056）是一种氨基核苷类抗生素，属于嘌呤霉素类似物，能可逆抑制二肽基肽酶和胞浆丙氨酸氨基肽酶，通过氧化应激依赖性调节ZO-1增加足细胞通透性，诱导细胞凋亡，并促进细胞迁移小体的分泌，常用于诱导肾病综合征模型的研究。

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。

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。

Omarigliptin 奥格列汀是一种有效的选择性口服二肽基肽酶 4 （DPP4） 抑制剂，IC50值为1.6nM。[3]

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.

Neuropeptide Y (3-36) (human, rat) is a metabolite of neuropeptide Y (NPY) generated by dipeptidyl peptidase-4 (DPP4). Known as a selective Y2 receptor agonist, Neuropeptide Y (3-36) (human, rat) effectively reduces the release of norepinephrine via the Y2 receptor[1][2].

Gly-Pro-pNA hydrochloride (Gly-Pro p-nitroanilide hydrochloride)是一种二肽基肽酶抑制剂，对二肽基肽酶II、二肽基肽酶IV和二肽基肽酶IX具有抑制作用。

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N CD13 (IC50 = 25 μM). It is selective for AP-N CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

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。

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].

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。

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.

Saxagliptin (BMS-477118) 是一种选择性，可逆性，竞争性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin 能够用于 2 型糖尿病的研究。

AZD-5248 is a potent, selective, first generation, oral inhibitor of dipeptidyl peptidase 1 (DPP1).

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。