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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 364611-21-2
- 화학식: C19H17N3S
- 분자량:319.42
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
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
-
CAS No. 364611-21-2
-
분자량 319.42
-
화학식 C19H17N3S
-
SMILES
C1(CCNC2=NC(C3=CNC4=C3C=CC=C4)=CS2)=CC=CC=C1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz