peptidase-a

Firibastat (RB150) 是一种具有口服活性的 EC33 前体药物。Firibastat 是一种首创的脑氨基肽酶 A(APA) 抑制剂 (Ki=200 nM)，选择性地抑制高血压大鼠脑血管紧张素 II 转化为血管紧张素 III，降低血压。

Carboxypeptidase A(EC 3.4.2.1) 是一种含锌的金属蛋白酶，常用于生化研究。Carboxypeptidase A 催化与多肽链 C 端相邻的肽键的水解。Carboxypeptidase A 是典型的金属蛋白酶，在生物系统中发挥重要作用。

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

P32 98 hemifumarate 是一种二肽基肽酶 IV (DPP4) 抑制剂，具有降血糖作用，可在 Zucker 糖尿病大鼠模型中可改善胰岛素敏感性和 β 细胞反应性，可用于研究2型糖尿病和结肠炎。

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

Imigliptin (KBP 3853) 是一种新型的二肽基肽酶-4 抑制剂，可用于研究2型糖尿病。

TS-021 是一种具有选择性的二肽基肽酶 4 (DPP-4) 抑制剂，具有抗糖尿病活性，可用于研究2 型糖尿病。

Leukotriene E4 (LTE4)（LTE4）通过 二肽酶对LTD4 上的作用生成，是过敏性休克慢反应物质（SRS-A）的成分之一。LTE4 存在于血浆和尿液中，可用于检测哮喘。

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。

Linagliptin (BI 1356) 是一种有效的、可口服的、基于二氢嘌呤二酮的二肽基肽酶 4 抑制剂，具有降血糖活性。

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。

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。

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。

Papain 是一种半胱氨酸蛋白酶，是肽酶 C1 家族中一员，在食品、医药、化妆品、纺织等具有广泛的应用。

Trelagliptin succinate (SYR-472 succinate) 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病(T2DM) 的研究。

Sitagliptin phosphate (MK-0431 phosphate) 是一种二肽基肽酶 4 (DPP4) 抑制剂，在 Caco-2 细胞中，IC50值为 19 nM。

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.

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

Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation. Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity.

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。

SPL-410 is a highly potent,selective and orally active inhibitor of hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a)(IC50 of 9 nM).

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.

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