T2M-010
T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD).
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- CAS. Nr.: 364611-21-2
- Formel: C19H17N3S
- Molecular Weight:319.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
T2M010 (25 µM, 1 h) leads to a robust twofold increase in SYK phosphorylation in HEK–hTREM2/DAP12 cells[1].
T2M-010 (25 µM, 30 min) significantly enhances bead uptake in BV2 cells, demonstrating a marked increase in phagocytic activity[1].
T2M-010 shows no cytotoxicity in human fibroblasts (WI-38 and HS-27; IC50 >100 µM), low hERG risk (IC50 > 60 µM), and minimal inhibition of major CYP isoforms at 10 µM (≤ 11.2%)[1].
T2M-010 can return robust A→B transport in MDCK– MDR1 assays (Papp = 2.85 × 10⁻⁵ cm/s) and a low efflux ratio (ER = 1.07), pointing to minimal P-gp–mediated efflux[1].
T2M-010 displays good gastrointestinal stability (> 88-86% parent remaining after 2 h in simulated gastric and intestinal fluids, respectively) and long plasma half-lives (167 min in mouse; 214 min in human)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 364611-21-2
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Molecular Weight 319.42
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Formel C19H17N3S
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SMILES
C1(CCNC2=NC(C3=CNC4=C3C=CC=C4)=CS2)=CC=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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