Asenapine
Based on 4 publication(s) in Google Scholar
Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.22%
- CAS. Nr.: 65576-45-6
- Formel: C17H16ClNO
- Molecular Weight:285.77
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Asenapine (Standard)5-HT/Dopamine/Histamine/Adrenergic Receptors Antagonist -
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8-OH-DPAT5-HT Receptor Agonist
Publications Citing Use of MedChemExpress (MCE) Asenapine
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Adrenergic Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Histamine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[4]|
5-HT1A Receptor 8.6 (pKi) |
5-HT1B Receptor 8.4 (pKi) |
5-HT2A Receptor 10.2 (pKi) |
5-HT2B Receptor 9.8 (pKi) |
5-HT2C Receptor 10.5 (pKi) |
5-HT5 Receptor 8.8 (pKi) |
5-HT6 Receptor 9.6 (pKi) |
5-HT7 Receptor 9.9 (pKi) |
Alpha-2A adrenergic receptor 8.9 (pKi) |
α1-adrenergic receptor 8.9 (pKi) |
Alpha-2B adrenergic receptor 9.5 (pKi) |
Alpha-2C adrenergic receptor 8.9 (pKi) |
D1 Receptor 8.9 (pKi) |
D2 Receptor 8.9 (pKi) |
D3 Receptor 9.4 (pKi) |
D4 Receptor 9.0 (pKi) |
H1 Receptor 9.0 (pKi) |
H2 Receptor 8.2 (pKi) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Wistar rats (200-250 g)[2]
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Dosage:0.05 mg/kg, 0.1 mg/kg, 0.2 mg/kg
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Administration:Subcutaneous injection
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Result:Produced suppression of CAR in a dose-dependent manner.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 65576-45-6
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Appearance Solid
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Molecular Weight 285.77
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Formel C17H16ClNO
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Color White to off-white
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SMILES
ClC1=CC=C2OC3=CC=CC=C3[C@@](C4)([H])[C@](CN4C)([H])C2=C1
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Synonyms
Org 5222
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Structural and expression analysis of the dopamine receptors reveals their crucial roles in regulating the insulin signaling pathway in oysters. [Abstract]2023 Aug 30:247:125703. PMID: 37414315 -
Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
Biomed Pharmacother
Identification of the atypical antipsychotic Asenapine as a direct survivin inhibitor with anticancer properties and sensitizing effects to conventional therapies. [Abstract]2025 Jan:182:117756. PMID: 39693907
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 200 mg/mL (699.85 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, 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.75 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 (8.75 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. M Shahid, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. [Content Brief]
[2]. Olivia Frånberg, et al. Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. [Content Brief]
[3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. [Content Brief]
[4]. Ene HM, et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91. [Content Brief]
[5]. Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. [Content Brief]
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 | 3.4993 mL | 17.4963 mL | 34.9927 mL | 87.4817 mL |
| 5 mM | 0.6999 mL | 3.4993 mL | 6.9985 mL | 17.4963 mL | |
| 10 mM | 0.3499 mL | 1.7496 mL | 3.4993 mL | 8.7482 mL | |
| 15 mM | 0.2333 mL | 1.1664 mL | 2.3328 mL | 5.8321 mL | |
| 20 mM | 0.1750 mL | 0.8748 mL | 1.7496 mL | 4.3741 mL | |
| 25 mM | 0.1400 mL | 0.6999 mL | 1.3997 mL | 3.4993 mL | |
| 30 mM | 0.1166 mL | 0.5832 mL | 1.1664 mL | 2.9161 mL | |
| 40 mM | 0.0875 mL | 0.4374 mL | 0.8748 mL | 2.1870 mL | |
| 50 mM | 0.0700 mL | 0.3499 mL | 0.6999 mL | 1.7496 mL | |
| 60 mM | 0.0583 mL | 0.2916 mL | 0.5832 mL | 1.4580 mL | |
| 80 mM | 0.0437 mL | 0.2187 mL | 0.4374 mL | 1.0935 mL | |
| 100 mM | 0.0350 mL | 0.1750 mL | 0.3499 mL | 0.8748 mL |
Asenapine Related Classifications
HY-10121 Related Classifications
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