Sipagladenant
Based on 1 Customer Validation
Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 858979-50-7
- Formula: C20H19N3O4S
- Molecular Weight:397.45
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve alternation behavior[2].
Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve gait parameters[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Medial prefrontal dopaminerjic terminal-lesioned CD(SD) IGS male rat[2]
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Dosage:0.3 mg/kg
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Administration:Oral administration; 0.3 mg/kg; once
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Result:Showed longer exploration time of the novel object (65.03%) than that of the familiar object (34.97%) (p<0.001).
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Animal Model:ICR mice with cognitive impairment and/or movement disoder[2]
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Dosage:0.1 mg/kg
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Administration:Oral administration; 0.1 mg/kg; once
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Result:Showed a significantly high alternation behavior (69.5%) as compared to the vehicle administration group (59.6%) (p<0.01).
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Animal Model:ICR mice with cognitive impairment and/or movement disoder[2]
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Dosage:0.1 mg/kg
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Administration:Oral administration; 0.1 mg/kg; once
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Result:Showed a significantly large maximum contact area and gait area of the left hindpaw as compared to the vehicle administration group (p<0.05), tendency of the maximum contact area and gait area of the right forepaw being large (p<0.1).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 858979-50-7
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Appearance Solid
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Molecular Weight 397.45
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Formula C20H19N3O4S
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Color Off-white to light yellow
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SMILES
O=C(C1=CN=C(C)C=C1)NC2=NC(C3=CC=CO3)=C(C(C4CCOCC4)=O)S2
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Synonyms
KW-6356
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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 : 50 mg/mL (125.80 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)
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 (6.29 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 | 2.5160 mL | 12.5802 mL | 25.1604 mL | 62.9010 mL |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0321 mL | 12.5802 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 mL | 6.2901 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6774 mL | 4.1934 mL | |
| 20 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1450 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0064 mL | 2.5160 mL | |
| 30 mM | 0.0839 mL | 0.4193 mL | 0.8387 mL | 2.0967 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5725 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2580 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4193 mL | 1.0483 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6290 mL |
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