AMG 333
Based on 1 Customer Validation
AMG 333 is an orally active and highly selective TRPM8 antagonist with an IC50 of 13 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 1416799-28-4
- Fòrmula: C20H12F5N3O4
- Peso molecular:453.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
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Actividad biológica
IC50: 13 nM (TRPM8)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Icilin (HY-11062)-induced wet-dog shake (WDS) behavior in Sprague−Dawley rat model[1]
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Dosage:0.6, 1, 3 mg/kg
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Administration:Oral gavage (p.o.), single dose
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Result:Demonstrated significant dose-dependent inhibition; 3 mg/kg fully inhibited WDS.
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Animal Model:Cold stimulation-induced blood pressure elevation Sprague−Dawley rat model[1]
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Dosage:1, 3 mg/kg
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Administration:Oral gavage (p.o.), single dose
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Result:Showed significant inhibition of cold-induced blood pressure elevation at 1 mg/kg and 3 mg/kg; 3 mg/kg fully blocked cold-pressor response.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1416799-28-4
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Appearance Solid
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Peso molecular 453.32
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Fòrmula C20H12F5N3O4
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Color White to off-white
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SMILES
FC1=CC=CN=C1[C@H](C2=CC(F)=C(OC(F)(F)F)C=C2)NC(C3=NC=C(C(O)=O)C=C3)=O
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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 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (275.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (4.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (4.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
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 (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2059 mL | 11.0297 mL | 22.0595 mL | 55.1487 mL |
| 5 mM | 0.4412 mL | 2.2059 mL | 4.4119 mL | 11.0297 mL | |
| 10 mM | 0.2206 mL | 1.1030 mL | 2.2059 mL | 5.5149 mL | |
| 15 mM | 0.1471 mL | 0.7353 mL | 1.4706 mL | 3.6766 mL | |
| 20 mM | 0.1103 mL | 0.5515 mL | 1.1030 mL | 2.7574 mL | |
| 25 mM | 0.0882 mL | 0.4412 mL | 0.8824 mL | 2.2059 mL | |
| 30 mM | 0.0735 mL | 0.3677 mL | 0.7353 mL | 1.8383 mL | |
| 40 mM | 0.0551 mL | 0.2757 mL | 0.5515 mL | 1.3787 mL | |
| 50 mM | 0.0441 mL | 0.2206 mL | 0.4412 mL | 1.1030 mL | |
| 60 mM | 0.0368 mL | 0.1838 mL | 0.3677 mL | 0.9191 mL | |
| 80 mM | 0.0276 mL | 0.1379 mL | 0.2757 mL | 0.6894 mL | |
| 100 mM | 0.0221 mL | 0.1103 mL | 0.2206 mL | 0.5515 mL |
AMG 333 Related Classifications
HY-112703 Related Classifications
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