peptidase-4

Gemigliptin Tartrate (LC15-0444 tartrate) 是一种选择性的，可逆的，竞争性的二肽基肽酶 4 (DPP-4) 抑制剂，对于人重组 DPP-4 的IC50=10.3 nM。Gemigliptin tartrate 具有很强的抗糖基化活性，能够用于晚期糖基化终产物相关的糖尿病并发症的研究。

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。

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。

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。

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。

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。

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。

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。

Alogliptin Benzoate (SYR 322) 是一种有效且特异性的 DPP-4 抑制剂 ，IC50值小于 10 nM，其选择性比 DPP-8 9 高 10,000 倍以上，可用于研究 2 型糖尿病。

Trelagliptin (SYR-472) 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。

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。

Anagliptin (SK-0403) 是一种选择性的二肽酰肽酶 4 抑制剂，IC50=3.8 nM，对 DPP-8 9 的选择性相对较弱，IC50分别为 68 和 60 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.

Talabostat mesylate (PT100) 是一种具有口服活性和非选择性的二肽基肽酶 IV 抑制剂(IC50< 4 nM;Ki= 0.18 nM)。Talabostat mesylate 是成纤维细胞活化蛋白的第一个临床抑制剂(IC50= 560 nM)，抑制 DPP8 9 (IC50= 4 11 nM;Ki= 1.5 0.76 nM)，静息细胞脯氨酸二肽酶(IC50= 310 nM)、DPP2 和一些其他 DASH 家族酶。Talabostat mesylate 具有抗肿瘤和造血刺激活性 。

DBPR108是新型、具有口服活性、选择性的DPP4抑制剂，IC50=为15nM，对DPP8和DPP9基本无抑制。

Dutogliptin (PHX-1149 free base) is an oral, effective and selective dipeptide-peptide-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.

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。

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。