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) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

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) , is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes)

AMG133 peptide payload serves as a GLP-1 agonist and is utilized as a peptide linker conjugate for AMG133.

AMG133 peptide payloadTFA is the trifluoroacetic acid (TFA) salt form of AMG133 peptide payload. This compound acts as a GLP-1 agonist and serves as a peptide-linker conjugate, which is utilized in the synthesis of AMG133.

Tezepelumab (AMG 157) is a humanized monoclonal antibody (IgG2λ) targeting TSLP that prevents TSLP from interacting with its heterodimer receptor. Tezepelumab can be used to study advanced asthma disease.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.

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

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

Tapotoclax (AMG-176) is an orally active MCL1 inhibitor for the study of myeloid leukemia.

PAMAM dendrimer G1.5 carboxylate (PAMAM G1.5 carboxylate) sodium is a polyanionic dendrimer composed of sodium terminal carboxylate groups. It has demonstrated antiviral activity in MERS-CoV plaque reduction assays, with an inhibition rate of 40.5%.

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) is a monoclonal antibody targeting hepatocyte growth factor that inhibits HGF/ MET-driven signaling. Rilotumumab has antitumor effects and can be used to study castration-resistant prostate cancer (CRPC) and gastric cancer.

AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.

AMG-119 is a humanized IgG1 monoclonal antibody that targets delta-like ligand 3 (DLL3). AMG-119 is applicable for research in relapsed/refractory (R/R) small cell lung cancer (SCLC).

AMG 118 Immobilized cephalosporin C acylase is an enzyme in immobilized form used primarily in industrial catalysis for the production of the vital pharmaceutical intermediate, 7-aminocephalosporanic acid (7-ACA). The CPC acylase it contains is a highly specialized β-lactam acylase or peptidase capable of cleaving the amide bond within β-lactams.