TREM2 agonist-2 (I-192) 是一种具有口服活性的髓系细胞触发受体 2 (triggering receptor expressed on myeloid cells-2, TREM2) 激动剂 (EC50<0.05 μM)。
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TREM2 agonist-2 (I-192) is an orally active triggering receptor expressed on myeloid cells 2 (TREM2) agonist (EC50<0.05 μM)[1].
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. |
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. |
[1]. Lara C. CZABANIUK, et al. Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use. WO2021226629A1.