TREM2 agonist-5
Based on 1 Customer Validation
TREM2 agonist-5 is the microglial lipid-sensing receptor (TREM2) agonist with a Kd of 71.36 μM. TREM2 agonist-5 is a racemic structural analog of the TREM2 agonist VG-3927 and exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells. TREM2 agonist-5 displays a superior in vitro pharmacokinetic profile to VG-3927. TREM2 agonist-5 can used for the study of Alzheimer’s disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.61%
- No. CAS: 3114105-24-4
- Fòrmula: C24H21ClFN5O
- Peso molecular:449.91
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
TREM-2 71.36 μM (Kd) |
In Vitro
TREM2 agonist-5 (Compound C1) displays a superior in vitro pharmacokinetic profile to VG-3927: enhanced metabolic stability in human and mouse liver microsomes, favorable passive permeability (PAMPA), and a central nervous system (CNS) -compatible log D7.4.[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3114105-24-4
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Appearance Solid
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Peso molecular 449.91
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Fòrmula C24H21ClFN5O
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Color White to off-white
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SMILES
CN1N=CC(C2C=C(C3=NC(C4=CC=C(Cl)C=C4F)=C(N=C(C)C(C)=N5)C5=C3)CCO2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (111.13 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. 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 |
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| DMSO | 1 mM | 2.2227 mL | 11.1133 mL | 22.2267 mL | 55.5667 mL |
| 5 mM | 0.4445 mL | 2.2227 mL | 4.4453 mL | 11.1133 mL | |
| 10 mM | 0.2223 mL | 1.1113 mL | 2.2227 mL | 5.5567 mL | |
| 15 mM | 0.1482 mL | 0.7409 mL | 1.4818 mL | 3.7044 mL | |
| 20 mM | 0.1111 mL | 0.5557 mL | 1.1113 mL | 2.7783 mL | |
| 25 mM | 0.0889 mL | 0.4445 mL | 0.8891 mL | 2.2227 mL | |
| 30 mM | 0.0741 mL | 0.3704 mL | 0.7409 mL | 1.8522 mL | |
| 40 mM | 0.0556 mL | 0.2778 mL | 0.5557 mL | 1.3892 mL | |
| 50 mM | 0.0445 mL | 0.2223 mL | 0.4445 mL | 1.1113 mL | |
| 60 mM | 0.0370 mL | 0.1852 mL | 0.3704 mL | 0.9261 mL | |
| 80 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6946 mL | |
| 100 mM | 0.0222 mL | 0.1111 mL | 0.2223 mL | 0.5557 mL |
TREM2 agonist-5 Related Classifications
HY-175510 Related Classifications
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