SYA16263
Based on 1 Customer Validation
SYA16263 is a dopamine D2 receptor (D2R) and serotonin 1A receptor (5-HT1AR) ligand, with Ki values of 1.24 nM and 0.67 nM for D2R and 5-HT1AR, respectively. SYA16263 stabilizes the inactive conformation of D2R and 5-HT1AR via interactions with specific amino acid residues in their orthosteric binding pockets, thereby blocking downstream signal transduction. SYA16263 can be used in research related to schizophrenia and psychosis.
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- Pureté : 99.35%
- CAS No.: 129281-28-3
- Formule: C19H24FN3
- Masse moléculaire:313.41
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
IC50 & Target
[1]|
Dopamine D2 receptor |
5-HT1AR |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SYA16263 (0.632-1.896 mg/kg; i.p.; single administration; 60-66 min) does not induce extrapyramidal side effects in the rat catalepsy test model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, ~6 weeks old, 133-153 g)[1]
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Dosage:0.632, 1.264, 1.896 mg/kg
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Administration:i.p.; single administration; 60, 63, 66 min
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Result:Did not induce extrapyramidal side effects
Chemical Information
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CAS No. 129281-28-3
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Appearance Solid
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Masse moléculaire 313.41
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Formule C19H24FN3
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Color White to off-white
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SMILES
FC(C=C1)=CC=C1CCCCN(CC2)CCN2C3=CC=CC=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (319.07 mM; Need ultrasonic; 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.98 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 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: ≥ 2.5 mg/mL (7.98 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.
Pureté et documentation
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Fiche technique (277 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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1907 mL | 15.9535 mL | 31.9071 mL | 79.7677 mL |
| 5 mM | 0.6381 mL | 3.1907 mL | 6.3814 mL | 15.9535 mL | |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1907 mL | 7.9768 mL | |
| 15 mM | 0.2127 mL | 1.0636 mL | 2.1271 mL | 5.3178 mL | |
| 20 mM | 0.1595 mL | 0.7977 mL | 1.5954 mL | 3.9884 mL | |
| 25 mM | 0.1276 mL | 0.6381 mL | 1.2763 mL | 3.1907 mL | |
| 30 mM | 0.1064 mL | 0.5318 mL | 1.0636 mL | 2.6589 mL | |
| 40 mM | 0.0798 mL | 0.3988 mL | 0.7977 mL | 1.9942 mL | |
| 50 mM | 0.0638 mL | 0.3191 mL | 0.6381 mL | 1.5954 mL | |
| 60 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3295 mL | |
| 80 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9971 mL | |
| 100 mM | 0.0319 mL | 0.1595 mL | 0.3191 mL | 0.7977 mL |