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.

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular 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.

Abrilumab (MEDI-7183) is a fully human monoclonal antibody against α4β7 that inhibits the α4β7 integrin and can be used to study inflammatory bowel disease and ulcerative colitis.

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.

Brazikumab (AMG 139) is a humanized antibody targeting IL-23 by binding to the P19 subunit. It is a selective IL23p19 antagonist and can be used in Crohn's disease research.

Solitomab (AMG 110) is a bispecific single-chain antibody targeting CD3 and EpCAM/CD326 (epithelial cell adhesion molecule), exhibiting in vitro activity against primary uterine carcinoma and ovarian sarcoma cell lines.

AMG 108 (MEDI 8968) is a fully human monoclonal antibody targeting IL-1R1, used in rheumatoid arthritis research.

Briquilimab (JSP-191) is a humanized, aglycosylated monoclonal antibody that directly inhibits the interaction between the stem cell factor (SCF) ligand and its receptor, KIT (CD117), leading to the blockade of the downstream KIT signaling pathway and ultimately inducing mast cell apoptosis; the SCF-KIT interaction is well-characterized as essential for mast cell survival, and its inhibition has been demonstrated to directly trigger mast cell apoptosis primarily through the Bim-mediated pathway, thereby removing the underlying cellular source of inflammation for many immunological and inflammatory diseases, including chronic urticaria and asthma.

Blinatumomab (AMG-10,MT-103) is a CD19/CD3 bispecific B-cell and T-cell binding antibody that directs T-cells to attack cancer cells by binding to both CD3 on T-cells and CD19 on cancer cells, and is used in acute lymphoblastic leukemia and non-Hodgkin's lymphoma.