amg1

AMG-1 is a specific CRAC channel inhibitor. AMG-1 blocks the function of effector T cells, but not regulatory T cells in vitro and it attenuates the progression and severity of EAE in vivo.

SYN1143 (AMG-1) 是人 RON 和 c-Met 的有效抑制剂。体外激酶测定表明 SYN1143 对人 RON 和 c-Met 的 IC50 分别为 9 和 4 nmol/L。

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.

AMG131 (CHS 131) 是一种新型非噻唑烷二酮(TZD) 选择性过氧化物酶体增殖物激活受体 (PPAR) γ 调节剂，可用于治疗 2 型糖尿病。

AMG133 peptide payload，作为一种GLP-1激动剂，被用于AMG133的肽连接剂缀合物。

AMG133 peptide payload TFA 是 AMG133 peptide payload 的 TFA 盐形式，它作为GLP-1激动剂，可以用于合成AMG133的肽-连接子偶合物。

Tezepelumab (AMG 157) 是一种人源化靶向 TSLP 的单克隆抗体 (IgG2λ)，阻止TSLP 与其异二聚体受体相互作用。Tezepelumab 可用于研究晚期哮喘疾病。

AMG-1694 是一种强效的葡萄糖激酶-葡萄糖激酶调节蛋白（GK-GKRP）干扰物，能促进 GK-GKRP 复合物的解离，其 IC50 值为 7 nM，从而间接提高 GK 酶的活性。AMG-1694 可使几种啮齿动物糖尿病模型的血糖水平恢复正常，并降低糖尿病动物而非正常血糖动物的血糖。AMG-1694 能有效逆转 GKRP 对 GK 活性的抑制作用，并促进 GK 转位。

ARRY-403 是一种新型葡萄糖激酶激活剂，可降低 2 型糖尿病患者的空腹和餐后血糖，可用于治疗糖尿病。

Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

Kira8 (AMG-18) 是一种单选择性 IRE1α 抑制剂，可变构减弱 IRE1α RNase 活性，IC50为 5.9 nM。

Tapotoclax (AMG-176) 是一种具有口服活性 MCL1 抑制剂，可用于研究髓系细胞白血病。

PAMAM dendrimer G1.5 carboxylate (PAMAM G1.5 carboxylate) sodium 是一种多聚阴离子树枝状聚合物，由端基羧酸钠组成。在MERS‐CoV斑块抑制试验中，PAMAM dendrimer G1.5 carboxylate 显示出40.5%的抗病毒活性。

AMG-126737 is an effective human lung mast cell trypsin inhibitor with potential therapeutic effect in lung diseases.

AMG-131 besylate is a hypoglycemic agent. It is a potent PPARγ partial agonist that displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs.

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK/Ay type 2 diabetic mice, effects that were sustained even after 12 h.

Rilotumumab (AMG 102) 是一种针对肝细胞生长因子的单克隆抗体，对 HGF/MET 驱动的信号传导有抑制作用。Rilotumumab 具有抗肿瘤作用，可用于研究去势抵抗性前列腺癌 (CRPC) 和胃癌。

AMG-193 是一种 MTA-PRMT5 复合物抑制剂，可用于研究癌症、呼吸系统疾病和消化系统疾病。

AMG-119 是一种靶向 delta 样配体 3 (DLL3) 的人源化 IgG1 单克隆抗体。AMG-119 适用于研究复发/难治性 (R/R) 小细胞肺癌 (SCLC)。

AMG 118 Immobilized cephalosporin C acylase 是一种用于催化的固定化酶，主要用于工业生产关键医药中间体7-氨基头孢烷酸 (7-ACA)。其内部的CPC acylase 是高特异性的β-内酰胺酰化酶或肽酶，能够断裂β-内酰胺环间的酰胺键。