AVN-101 hydrochloride
Based on 1 Customer Validation
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.06%
- CAS. Nr.: 1061354-48-0
- Formel: C21H25ClN2
- Molecular Weight:340.89
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-HT2A Receptor |
5-HT2C Receptor |
5-HT6 Receptor |
5-HT7 Receptor |
5-HT7 Receptor 0.153 nM (Ki) |
5-HT2C Receptor 1.17 nM (Ki) |
5-HT2A Receptor 1.56 nM (Ki) |
5-HT6 Receptor 2.04 nM (Ki) |
5-HT2B Receptor 10.6 nM (Ki) |
5-HT1A Receptor 61 nM (Ki) |
5-HT1B Receptor 720 nM (Ki) |
H1 Receptor 0.58 nM (Ki) |
Alpha-2B adrenergic receptor 0.41 nM (Ki) |
Alpha-2A adrenergic receptor 1.77 nM (Ki) |
Alpha-2C adrenergic receptor 3.55 nM (Ki) |
Alpha-1B adrenergic receptor 9.4 nM (Ki) |
Alpha-1A adrenergic receptor 18.9 nM (Ki) |
Alpha-1D adrenergic receptor 30.2 nM (Ki) |
In Vitro
AVN-101 hydrochloride shows some ability to compete with radio-labeled ligands for both the histamine H1 (Ki = 0.58 nM) and H2 receptors (Ki = 89 nM) while being totally inactive on H3 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AVN-101 (0.02-5 mg/kg; i.p.; once) hydrochloride prevents Scopolamine (HY-N0296)-induced amnesia in a passive avoidance test in mice when administered at a dose of 0.05 mg/kg[1].
AVN-101 (0.2, 1, and 5 mg/kg) hydrochloride increases the time spent in the open arms of the elevated plus maze in mice[1].
AVN-101 hydrochloride is poorly stable in murine plasma: by the end of 30-min incubation at room temperature, the residual amount of the original compound is reduced to 16%. At the same time, AVN-101 hydrochloride shows better stability in plasma samples taken from monkey and human: by the end of the 30-min incubation at room temperature, the residual amount of the original compound is reduced to only 45% and 68%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/C mice bearing porsolt forced swim and the tail suspension tests[1]
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Dosage:0.05 mg/kg
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Administration:i.p.; once daily; for 4 days
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Result:Reduced immobility in the forced swim test in mice.
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Animal Model:Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment[1].
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Dosage:0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
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Administration:i.p.; once
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Result:Prevented scopolamine-induced amnesia in a passive avoidance test in mice.
Chemical Information
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CAS. Nr. 1061354-48-0
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Appearance Solid
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Molecular Weight 340.89
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Formel C21H25ClN2
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Color White to light yellow
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SMILES
CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CC=CC=C4.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (366.69 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). 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). 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)
Reinheit & Dokumentation
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Data Sheet (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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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). 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 | 2.9335 mL | 14.6675 mL | 29.3350 mL | 73.3374 mL |
| 5 mM | 0.5867 mL | 2.9335 mL | 5.8670 mL | 14.6675 mL | |
| 10 mM | 0.2933 mL | 1.4667 mL | 2.9335 mL | 7.3337 mL | |
| 15 mM | 0.1956 mL | 0.9778 mL | 1.9557 mL | 4.8892 mL | |
| 20 mM | 0.1467 mL | 0.7334 mL | 1.4667 mL | 3.6669 mL | |
| 25 mM | 0.1173 mL | 0.5867 mL | 1.1734 mL | 2.9335 mL | |
| 30 mM | 0.0978 mL | 0.4889 mL | 0.9778 mL | 2.4446 mL | |
| 40 mM | 0.0733 mL | 0.3667 mL | 0.7334 mL | 1.8334 mL | |
| 50 mM | 0.0587 mL | 0.2933 mL | 0.5867 mL | 1.4667 mL | |
| 60 mM | 0.0489 mL | 0.2445 mL | 0.4889 mL | 1.2223 mL | |
| 80 mM | 0.0367 mL | 0.1833 mL | 0.3667 mL | 0.9167 mL | |
| 100 mM | 0.0293 mL | 0.1467 mL | 0.2933 mL | 0.7334 mL |
AVN-101 hydrochloride Related Classifications
HY-117046A Related Classifications
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