您当前的位置:

信号通路

-收起全部分类

Dipeptidyl Peptidase

Dipeptidyl Peptidase相关产品(22)
货号 产品名 中文名称 产品描述
SJ-MX3281 Trelagliptin (SYR-472) succinate 曲格列汀琥珀酸盐 Trelagliptin succinate (SYR-472) is a selective, long acting dipeptidyl peptidase-4 (DPP-4) inhibitor. An antidiabetic agent.
SJ-MX3493 DBPR108 DBPR108 is a novel, potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; It shows no inhibition on DDP8 and DPP9. The in vivo effects of DBPR108, including inhibition of plasma DPP-IV activity and suppression of blood glucose elevation, were also demonstrated. As a potent, selective, long-acting and safe DPP-IV inhibitor, DBPR108 has the potential to be developed as a therapeutic for the treatment of type 2 diabetes mellitus.
SJ-MX3658 Brensocatib (AZD7986) Brensocatib (AZD7986) is a highly potent, reversible, and selective DPP1 inhibitor (pIC50 value of 8.4). Moreover, good species crossover was seen with the DPP1 enzyme (pIC50 values of 7.6, 7.7, 7.8 and 7.8 for mouse, rat, dog and rabbit, respectively). Clinical candidate for COPD.
SJ-MX1943A Sitagliptin phosphate monohydrate 西他列汀磷酸盐一水合物 Sitagliptin (MK0431 phosphate monohydrate) 是一种有效的 DPP4 抑制剂,在 Caco-2 细胞中,IC50 值为 19 nM。
SJ-MX1943B Sitagliptin phosphate 磷酸西他列汀 Sitagliptin phosphate (MK431; Januvia), the phosphate salt of Sitagliptin, is an antihyperglycemic agent (sugar-lowering) and antidiabetic medication that act as a potent inhibitor of DPP-IV (dipeptidyl peptidase-4) with IC50 of 19 nM in Caco-2 cell extracts.
SJ-MX3468 Teneligliptin hydrobromide Teneligliptin hydrobromide is a highly potent, selective, long-lasting and orally active DPP-4 inhibitor with in vitro IC50 values of 0.37 nM (human) and 0.29 nM (rat).
SJ-MX1016 Talabostat mesylate

Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) 是一种口服活性和非选择性的二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50 < 4 nM; Ki = 0.18 nM) 。Talabostat mesylate是成纤维细胞活化蛋白 (FAP) 的第一个临床抑制剂 (IC50 = 560 nM),抑制 DPP8和DPP9(IC50=4和11 nM,Ki =1.5和0.76 nM),静息细胞脯氨酸二肽酶 (QPP) (IC50=310 nM)、DPP2 和一些其他 DASH 家族酶,具有抗肿瘤和造血刺激活性 。

SJ-MX2217 Nateglinide 那格列奈 Nateglinide 是 D-苯丙氨酸的一个衍生物,是一种具有口服活性的、短效的促胰岛素释放化合物,也是 DPP IV 的抑制剂。 Nateglinide 抑制胰岛β细胞中 ATP 敏感的 K+ 通道。Nateglinide 可用于 2 型糖尿病 (非胰岛素依赖的) 的研究。
SJ-MX2417 Omarigliptin(MK-3102) 奥格列汀 Omarigliptin(MK-3102)是DPP4高效选择性抑制剂,IC50值为1.6nM。
SJ-MX2266 NDMC101 NDMC101 是一种有效的破骨细胞形成 (osteoclastogenesis) 抑制剂,通过下调 NFATc1 调控基因表达抑制破骨细胞分化。NDMC101 与 DPP4 底物相似,并且通过抑制 DPP4 而抑制早期 T 细胞激活的重要抑制剂。NDMC101 可用于骨疾病的研究,如类风湿关节炎、滑膜炎等。
SJ-MX2418 Saxagliptin (BMS-477118) 沙格列汀 Saxagliptin (BMS-477118) 是一种有效,选择性,可逆,竞争性和具有口服活性的二肽基肽酶 4 (DPP-4) (Ki = 0.6-1.3 nM) 抑制剂。Saxagliptin 可用于 2 型糖尿病的研究。
SJ-MX1943 Sitagliptin 西格列汀 Sitagliptin (MK-0431) 是一种有效的 DPP4 抑制剂,在 Caco-2 细胞中,IC50 值为 19 nM。
SJ-MX1872 Alogliptin (SYR-322 free base) 阿格列汀 Alogliptin (SYR-322 free base) 是一种有效的、具有选择性口服活性的 DPP-4 的抑制剂,IC50 值小于 10 nM,比对 DPP-8 和 DPP-9 的抑制性高 10000 倍以上。Alogliptin 可用于研究 2 型糖尿病。
SJ-MX1872A Alogliptin Benzoate 苯甲酸阿格列汀 Alogliptin Benzoate (SYR-322) is a potent, selective inhibitor of DPP-4 (dipeptidyl peptidase-4) with an IC50 of <10 nM. Displays greater than 10,000-fold selectivity over DPP-8 and DPP-9. An anti-diabetic agent for treatment of type 2 diabetes.
SJ-MX0909 Linagliptin 利拉利汀

Linagliptin是竞争性和高度选择性的二肽基肽酶 (DPP)-4 抑制剂(体外IC50 值 1 nM),在体内具有超强的效力和较长的作用持续时间。 Linagliptin对 DPP4 的选择性比 DPP-8、DPP-9、氨基肽酶 N 和 P、脯氨酰寡肽酶、胰蛋白酶、纤溶酶和凝血酶的选择性高 10,000 倍以上,比体外成纤维细胞活化蛋白的选择性高 90 倍。 临床研究中,Linagliptin被批准用于治疗 2 型糖尿病,通过控制 GLP-1 和胰岛素对葡萄糖耐量具有长期影响。

SJ-MX1874 Vildagliptin 维达列汀 Vildagliptin (LAF237) 是一种有效且稳定的选择性二肽基肽酶IV (DPP-IV) 抑制剂,在人 Caco-2 细胞中抑制 DPP-IV 的 IC50 为 3.5 nM。Vildagliptin 具有出色的口服生物利用度和有效的降血糖活性。
SJ-MX2418A Saxagliptin hydrate Saxagliptin hydrate (also known as BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate; brand name: Onglyza), the hydrate form of Saxagliptin, is a potent, orally bioactive, selective and reversible DPP4 (dipeptidyl peptidase-4) inhibitor with IC50 of 26 nM. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation.
SJ-MX4310 UAMC00039 dihydrochloride UAMC00039 dihydrochloride is a novel, potent, reversible and competitive dipeptidyl peptidase II (DPP-II) inhibitor with an IC50 of 0.48 nM. UAMC 00039 dihydrochloride demonstrates selectivity for DPP-II against DPP-9, DPP-8 and DPP-IV (IC50 values are 78.6, 142 and 165 μM, respectively).
SJ-MX4588 Anagliptin Anagliptin (formerly known as SK0403) is a novel, potent, orally bioactive, highly selective inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC50 of 3.8 nM. It is less selective against DPP-8/9 (IC50 = 68, 60 nM).
SJ-MX2418B Saxagliptin hydrochloride Saxagliptin hydrochloride  (BMS-477118 hydrochloride)  is a potent, orally bioactive, selective and reversible DPP4 (dipeptidyl peptidase-4) inhibitor with IC50 of 26 nM.