| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
As48 (0.1-1000 μM; 10 min) directly binds to recombinant human TREM2 protein, with a K0 value of 12.48 μM, as determined by the TRIC binding assay [1]. As48 (0.01-100 μM; 10 min) binds to recombinant human TREM2 protein, with a KD value of 13.8 μM, and its binding affinity to recombinant human TREM1 protein is 7 times weaker (KD = 97.92 μM), as determined by the MST binding assay [1]. As48 (30 μM; 20 min) can increase the thermal stability of recombinant human TREM2 protein by 3.86°C, as determined by the thermal displacement assay [1]. As48 (1.23-100 μM) directly binds to biotin-labeled recombinant human TREM2 protein, with a KD value of 29.5 μM, as determined by the SPR binding assay [1]. As48 (0-300 μM; overnight) showed extremely low cytotoxicity to HMC3 human microglia, and MTS assay showed no significant decrease in cell viability at concentrations up to 100 μM [1]. As48 (5-100 μM; 5-60 min) activated the TREM2 signaling pathway in HEK293-hTREM2/DAP12 cells by inducing dose- and time-dependent SYK phosphorylation [1]. As48 (0.3-30 μM; 10 min) induced TREM2-dependent intracellular calcium mobilization in HEK293-hTREM2/DAP12 cells [1]. As48 (0.3-30 μM; 0-120 min) activated the TREM2 signaling pathway in HMC3 TREM2-overexpressing human microglia by inducing dose- and time-dependent SYK phosphorylation [1]. As48 (25 μM; 30 min) increased the phagocytic activity of microglia in BV2 mice by two times compared with the solvent control group, as determined by a fluorescent latex bead uptake assay [1]. As48 (1-30 μM; 18 h) inhibited the shedding of the extracellular domain of TREM2 in HEK293-TREM2 overexpressing cells in a dose-dependent manner [1]. As48 (10-300 μM; 30 min) did not inhibit the proteolytic activity of recombinant human ADAM10 or ADAM17 at concentrations up to 300 μM, as determined by a fluorescent protease activity assay [1].
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: HMC3 human microglia Tested Concentrations: 0, 3, 10, 30, 100, 300 μM Incubation Duration: Overnight Experimental Results: No significant cytotoxicity was observed at concentrations up to 100 μM; cell viability was reduced by approximately 20% at 300 μM. Western Blot Analysis [1] Cell Types: HMC3 human microglia stably overexpressing TREM2 (HMC3 TREM2 OE cells) Tested Concentrations: 0.3, 1, 3, 10, 30 μM Incubation Duration: 5, 10, 30, 60, 120 minutes Experimental Results: Induction of dose- and time-dependent SYK phosphorylation. Western Blot Analysis [1] Cell Types: HEK293 cells stably overexpressing TREM2 (HEK293-TREM2 OE cells) Tested Concentrations: 1, 3, 10, 30 μM Incubation Duration: 18 hours Experimental Results: The protective effect of the extracellular domain of TREM2 was dose-dependent. Concentrations above 10 μM significantly inhibited its shedding, with the best effect observed at 30 μM. At 3 μM, the level of soluble TREM2 in the conditioned medium decreased to a level comparable to GM6001 (30 μM) without affecting APP secretion. |
| References |
| Molecular Formula |
C20H15N3OS
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|---|---|
| Molecular Weight |
345.42
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| CAS # |
1214405-38-5
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| Appearance |
Light brown to gray solid
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿和光照下。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8950 mL | 14.4751 mL | 28.9503 mL | |
| 5 mM | 0.5790 mL | 2.8950 mL | 5.7901 mL | |
| 10 mM | 0.2895 mL | 1.4475 mL | 2.8950 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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