As48
Based on 1 Customer Validation
As48 is a selective TREM2 agonist with a KD value of 12.48 μM in TRIC binding assay. As48 binds near the TREM2 cleavage region, forms hydrogen bonds with Gly68, reduces conformational flexibility in regions 58-102, restricts protease accessibility to the cleavage site. As48 activates SYK phosphorylation, enhances microglial phagocytosis, and induces downstream calcium signaling in TREM2-expressing cells. As48 inhibits TREM2 ectodomain shedding without affecting ADAM10/17 protease activities. As48 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 1214405-38-5
- Formula: C20H15N3OS
- Molecular Weight:345.42
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
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TREM-2 12.48 μM (Kd) |
As48 (0.1-1000 μM; 10 min) binds directly to recombinant human TREM2 protein with a K0 of 12.48 μM, as measured by TRIC binding assay[1].
As48 (0.01-100 μM; 10 min) binds to recombinant human TREM2 with a KD of 13.8 μM, and binds 7-fold more weakly to recombinant human TREM1 (KD = 97.92 μM), as measured by MST binding assay[1].
As48 (30 μM; 20 min) increases the thermal stability of recombinant human TREM2 protein by +3.86°C, as measured by thermal shift assay[1].
As48 (1.23-100 μM) binds directly to biotinylated recombinant human TREM2 protein with a KD of 29.5 μM, as measured by SPR binding assay[1].
As48 (0-300 μM; overnight) exhibits minimal cytotoxicity in HMC3 human microglial cells, with no significant viability loss at concentrations up to 100 μM, as measured by MTS assay[1].
As48 (5-100 μM; 5-60 min) activates TREM2 signaling in HEK293-hTREM2/DAP12 cells by inducing dose- and time-dependent SYK phosphorylation[1].
As48 (0.3-30 μM; 10 min) induces TREM2-dependent intracellular calcium mobilization in HEK293-hTREM2/DAP12 cells[1].
As48 (0.3-30 μM; 0-120 min) activates TREM2 signaling in HMC3 TREM2 OE human microglial cells by inducing dose- and time-dependent SYK phosphorylation[1].
As48 (25 μM; 30 min) enhances phagocytic activity in BV2 murine microglial cells by twofold compared to vehicle control, as measured by fluorescent latex bead uptake assay[1].
As48 (1-30 μM; 18 h) inhibits TREM2 ectodomain shedding in HEK293-TREM2 OE cells in vitro in a dose-dependent manner[1].
As48 (10-300 μM; 30 min) does not inhibit the proteolytic activity of recombinant human ADAM10 or ADAM17 at concentrations up to 300 μM, as measured by fluorogenic protease activity assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMC3 human microglial cells
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Concentration:0, 3, 10, 30, 100, 300 μM
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Incubation Time:overnight
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Result:Showed no significant cytotoxicity at concentrations up to 100 μM; Showed ~20% reduction in cell viabilityat 300 μM.
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Cell Line:HMC3 human microglial cells stably overexpressing TREM2 (HMC3 TREM2 OE cells)
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Concentration:0.3, 1, 3, 10, 30 μM
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Incubation Time:5, 10, 30, 60, 120 min
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Result:Induced dose- and time-dependent SYK phosphorylation.
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Cell Line:HEK293 cells stably overexpressing TREM2 (HEK293-TREM2 OE cells)
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Concentration:1, 3, 10, 30 μM
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Incubation Time:18 h
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Result:Showed dose-dependent preservation of the TREM2 extracellular domain, with significant protection against shedding at concentrations above 10 μM and maximal effect at 30 μM.
Reduced soluble TREM2 levels in conditioned media to a magnitude comparable to GM6001(HY-15768) (30 μM) at 3 μM, with no effect on APP secretion.
Chemical Information
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CAS No. 1214405-38-5
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Appearance Solid
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Molecular Weight 345.42
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Formula C20H15N3OS
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Color Light brown to gray
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SMILES
O=C(N1C2=C(CC1)C=C(C3=CN4C=CC=CC4=N3)C=C2)C5=CC=CS5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 1 mg/mL (2.90 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8950 mL | 14.4751 mL | 28.9503 mL | 72.3757 mL |