TREM2 agonist-2

Names

[ CAS No. ]:
2738485-98-6

[ Name ]:
TREM2 agonist-2

Biological Activity

[Description]:

TREM2 agonist-2 (I-192) is an orally active triggering receptor expressed on myeloid cells 2 (TREM2) agonist (EC50<0.05 μM)[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[In Vitro]

TREM2 agonist-2 (0-100 μM; 16 h) treatment activates hTREM2 in HEK293 cell[1]. Cell Viability Assay[1] Cell Line: HEK293 cells Concentration: 0-100 μM Incubation Time: 16 hours Result: Showed an EC50 value <0.05 μM.

[In Vivo]

TREM2 agonist-2 (oral gavage; 50 mg/kg; twice daily; one day) finds TREM2 target engagement on microglia[1]. Animal Model: Transgenic mice knock-in hTREM2-CV[1] Dosage: 50 mg/kg Administration: Oral gavage; 50 mg/kg; twice daily; one day Result: Increased genes associated with the adaptive immune response, innate immune response, microglia function, cytokine signalling, and cell cycle in hippocampus from animals.

[References]

[1]. Lara C. CZABANIUK, et al. Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use. WO2021226629A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H23ClFN5O

[ Molecular Weight ]:
451.92


Related Compounds