trem2

TREM2 agonist-2 (I-192) is an orally active and potent agonist of myeloid triggered receptor 2 (TREM2) for neurodegenerative disease research.

PY314 is a CHO-expressed humanized monoclonal antibody targeting TREM2 with antitumor activity for the study of metastatic renal cell carcinoma.

TREM2 agonist-1 (I-246) is a triggering receptor expressed on myeloid cells-2 (TREM2) agonist with an EC50 ranging from 3.0 μM to 100 μM.

TREM2 agonist-3 (Compound 4i) is a direct TREM2 agonist (Kd=19.0 µM), and its Kd value for TREM1 is 39.8 µM. It induces Syk phosphorylation and enhances microglial cell phagocytosis, and can be used for the study of neurodegenerative diseases.

TREM2 agonist-4 (Compound 4a) is a TREM2 agonist with a Kd value of 45.9 μM. It activates the TREM2 downstream signaling pathways and enhances the phagocytic function of microglia. TREM2 agonist-4 is applicable for research into neurodegenerative diseases such as Alzheimer's disease.

TREM2 agonist-5 is a ligand for the microglial lipid-sensing receptor (TREM2) and acts as an agonist with a Kd of 71.36 μM. It is the racemic analog of the TREM2 agonist VG-3927 and demonstrates excellent microglial phagocytic activity in HEK293-hTREM2/DAP12 cells, effectively activating TREM2 signaling. TREM2 agonist-5 has superior in vitro pharmacokinetics compared to VG-3927 and is potentially useful for Alzheimer's disease research.

TREM2-IN-1 (OPA) is a platinum-based TREM2 inhibitor with anti-cancer activity, blocking DNA replication and inhibiting TREM2 on myeloid cells. It suppresses immune regulatory activity, reducing CD206 and CX3CR1 in a mouse model of colorectal cancer.

rel-5-(4-Chloro-2-fluorophenyl)-2,3-dimethyl-7-[(2R,4S)-tetrahydro-2-(1-methyl-1H-pyrazol-4-yl)-2H-pyran-4-yl]pyrido[3,4-b] The EC50 value of pyrazine against TREM2 was ≤ 0.05 μM and the E.max value was > 250 μM.

Anti-TREM2 Antibody (AL2p-58) is a humanized IgG1 monoclonal antibody targeting TREM2.

IA9 (human TREM-2 182-190) is a TREM-2 inhibitor that can reduce the release of pro-inflammatory factors in collagen-induced arthritis mice, effectively suppressing joint inflammation and damage.

IA9 TFA (human TREM-2 182-190 TFA) is a TREM-2 inhibitor that reduces the release of pro-inflammatory cytokines in mice with collagen-induced arthritis, significantly suppressing joint inflammation and damage.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.

Iluzanebart, a human monoclonal IgG1 antibody, functions as an agonist antibody for human TREM2 (hTREM2), thereby enhancing the survival and overall function of microglia through the activation of the TREM2 signaling pathway. Iluzanebart provides compensation for the loss of CSF1R function, and it can be employed as a research agent for adult-onset leukoencephalopathy associated with CSF1R (colony stimulating factor 1 receptor) (CSF1R-ALSP), thereby providing opportunities to model microglial dysfunction in neurodegenerative disorders.

EP4 antagonist 14 is a prostaglandin E2 receptor subtype EP4 antagonist, demonstrating an IC50 of 1.1 nM in a HEK293 human receptor reporter assay and blocking β-arrestin recruitment due to PGE2 with an IC50 of 0.9 nM. At 10 µM, it reduces PGE2-stimulated mRNA levels of Il-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1) in RAW 264.7 macrophages. When used at 30 mg/kg per day alongside anti-PD-1 antibodies, it curbs tumor growth and enhances CD8+ T cell infiltration in tumors using a CT26 murine colon cancer model.

EOS006215 is a humanized monoclonal antibody inhibitor targeting TREM-2. It has the ability to reprogram TREM2+ macrophages, significantly hindering their tumor-promoting activities and overcoming drug resistance. In mouse models with orthotopic 4T1 triple-negative breast cancer, EOS006215 reduces metastatic burden. Additionally, it notably inhibits tumor growth in anti-PD-1 resistant mouse models. EOS006215 is applicable for studies on triple-negative breast cancer (TNBC).

AL002 is a humanized monoclonal immunoglobulin G1 (IgG1) antibody and acts as a TREM2 agonist antibody, suitable for research in neurological disorders.