AP521
Based on 1 Customer Validation
AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.96%
- CAS. Nr.: 151227-08-6
- Formel: C20H19ClN2O3S
- Molecular Weight:402.89
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Speicherung:
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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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5-HT1A Receptor 94 nM (IC50, in human) |
5-HT1A Receptor |
5-HT1A Receptor 135 nM (IC50, in rat) |
5-HT1B Receptor 254 nM (IC50, in rat) |
5-HT1B Receptor 5530 nM (IC50, in human) |
5-HT1D Receptor 418 nM (IC50, in human) |
5-HT5A Receptor 422 nM (IC50, in human) |
5-HT7 Receptor 198 nM (IC50, in rat) |
AP521 is an agonist of human 5-HT1A receptor with IC50s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT1A (rat), 5-HT1A (human), 5-HT1B (rat), 5-HT1B (human), 5-HT1D (human), 5-HT5a (human) and 5-HT7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 151227-08-6
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Appearance Solid
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Molecular Weight 402.89
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Formel C20H19ClN2O3S
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Color White to off-white
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SMILES
O=C([C@H]1CC(C2=CC=CC=C2S3)=C3CN1)NCC4=CC=C(OCO5)C5=C4.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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)
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (62.05 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 (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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.21 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 (6.21 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.
Protokoll
Membranes of neurotransmitter receptors are prepared from the tissues of rat, mouse, and guinea pig or from recombinant cells. These membranes are incubated in assay buffers containing selective radioligand for each receptor and AP521. After the incubation, the mixture is vacuum filtered through a glass membrane filter and washed by cold reaction buffer. Afterward, the radioactivity of the filters is counted[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male Sprague-Dawley rats weighing 250 to 300 g are anesthetized with pentobarbital sodium (50 mg/kg, i.p.) and placed on a stereotaxic apparatus. Dialysis probes with an outer diameter of 0.105 mm are inserted into the guide cannulae so that 3.0 mm of the probes are exposed to the tissue of the medial prefrontal cortex. Rats are housed individually after these operations. On the following day, perfusion is started in the home cage using artificial cerebrospinal fluid (145 mM NaCl, 3.0 mM KCl, 1.3 mM CaCl2, 1.0 mM MgCl2) at a flow rate of 2 mL/min. AP521 (3, 10 mg/kg), tandospirone (10 mg/kg) or vehicle are administered subcutaneously 60 min after sample collection started. The dialysate samples are collected every 30 min for 180 min and extracellular levels of 5-HT are determined[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
Verweise
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 | 2.4821 mL | 12.4103 mL | 24.8207 mL | 62.0517 mL |
| 5 mM | 0.4964 mL | 2.4821 mL | 4.9641 mL | 12.4103 mL | |
| 10 mM | 0.2482 mL | 1.2410 mL | 2.4821 mL | 6.2052 mL | |
| 15 mM | 0.1655 mL | 0.8274 mL | 1.6547 mL | 4.1368 mL | |
| 20 mM | 0.1241 mL | 0.6205 mL | 1.2410 mL | 3.1026 mL | |
| 25 mM | 0.0993 mL | 0.4964 mL | 0.9928 mL | 2.4821 mL | |
| 30 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0684 mL | |
| 40 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5513 mL | |
| 50 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2410 mL | |
| 60 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0342 mL |
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