Targetmol Chemicals Inc. | USA | Inquire | ||
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Chemical manufacturer since 2013 | ||||
chemBlink standard supplier since 2025 | ||||
Classification | Organic raw materials >> Organic fluorine compound |
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Name | TREM2 agonist-2 |
Synonyms | 5-(4-chloro-2-fluorophenyl)-2,3-dimethyl-7-[(2R,4S)-2-(1-methylpyrazol-4-yl)oxan-4-yl]pyrido[3,4-b]pyrazine |
Molecular Structure | ![]() |
Molecular Formula | C24H23ClFN5O |
Molecular Weight | 451.92 |
CAS Registry Number | 2738485-98-6 |
SMILES | CC1=NC2=CC(=NC(=C2N=C1C)C3=C(C=C(C=C3)Cl)F)[C@H]4CCO[C@H](C4)C5=CN(N=C5)C |
SDS | Available |
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TREM2 agonist-2 is a synthetic small-molecule compound developed as a pharmacological activator of the triggering receptor expressed on myeloid cells 2 (TREM2), a membrane-bound receptor primarily expressed on microglia in the central nervous system and other tissue-resident macrophages. TREM2 is involved in modulating the innate immune response, phagocytosis, lipid metabolism, and cellular survival pathways. The interest in TREM2 as a therapeutic target grew significantly after genetic studies linked variants in the TREM2 gene to an increased risk for neurodegenerative diseases such as Alzheimer’s disease. These findings encouraged the search for small molecules or biologics capable of activating TREM2 signaling. TREM2 agonist-2 emerged from high-throughput screening campaigns designed to identify low-molecular-weight compounds that could activate TREM2-dependent signaling cascades in microglial cells. The compound was selected based on its capacity to enhance TREM2-mediated phosphorylation events, particularly those involving the downstream adaptor DAP12 and SYK kinase, which are required for TREM2’s immune-modulatory effects. Biochemical assays confirmed that TREM2 agonist-2 binds selectively to the TREM2 receptor or its associated complex, leading to activation of canonical intracellular signaling pathways and transcriptional changes in immune-related genes. In preclinical cellular models, TREM2 agonist-2 demonstrated the ability to stimulate microglial functions including phagocytosis of apoptotic debris, uptake of aggregated amyloid-β, and secretion of neuroprotective cytokines. These properties positioned the compound as a candidate for further exploration in animal models of neurodegeneration. In vivo administration of TREM2 agonist-2 in rodent models of Alzheimer’s disease showed increased microglial clustering around amyloid plaques, reduction in plaque burden, and improvement in behavioral deficits associated with memory and cognition. Such effects were found to be TREM2-dependent, as they were abolished in knockout models lacking functional TREM2 protein. The compound has also been evaluated for its potential immunomodulatory effects outside of the central nervous system. TREM2 expression is relevant in certain tumor-associated macrophages and in inflammatory pathologies involving myeloid cells. Preliminary studies have indicated that TREM2 agonist-2 can influence the phenotype of macrophages in vitro, leading to upregulation of genes associated with tissue remodeling and immune homeostasis. However, the majority of its pharmacological characterization to date has focused on its central nervous system applications. Pharmacokinetic profiling of TREM2 agonist-2 has shown favorable oral bioavailability and adequate blood-brain barrier penetration in animal models. Toxicology studies in rodents and nonhuman primates revealed no dose-limiting adverse effects over subchronic dosing periods. The pharmacological profile of TREM2 agonist-2 indicates its potential for use in chronic diseases where modulation of microglial function may be beneficial, especially in neurodegenerative contexts characterized by impaired clearance of toxic protein aggregates and defective innate immune signaling. TREM2 agonist-2 remains under preclinical development, and to date, it has not entered human clinical trials. Nonetheless, the compound is frequently used in laboratory research to investigate the therapeutic potential of TREM2 activation and to validate TREM2 as a target in Alzheimer’s disease and other disorders of neuroinflammation. The development of TREM2 agonist-2 has contributed significantly to the understanding of microglial biology and immune mechanisms in the brain. Continued studies are expected to clarify its full pharmacological spectrum and inform the future design of clinical candidates targeting the TREM2 pathway. |
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List of Reports Available for TREM2 agonist-2 |