Azaphen dihydrochloride monohydrate
Based on 1 publication(s) in Google Scholar
Azaphen dihydrochloride monohydrate is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen dihydrochloride monohydrate increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen dihydrochloride monohydrate can be used in studies related to depression.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 63302-99-8
- Formula: C16H23Cl2N5O2
- Molecular Weight:388.29
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Publications Citing Use of MedChemExpress (MCE) Azaphen dihydrochloride monohydrate
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Biological Activity
Description
In Vitro
Azaphen (5-20 mg/kg; p.o.; single dose) dihydrochloride monohydrate (Azafen dihydrochloride monohydrate) exhibits pronounced antidepressant activity in the Porsolt behavioral despair test, with significant reductions in immobility duration at oral doses of 5, 10, and 20 mg/kg[2].
Azaphen dihydrochloride monohydrate exhibits pronounced antidepressant activity in the Normura forced swimming test with significant reductions in depressive state duration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Azaphen dihydrochloride monohydrate binds preferentially to the allosteric (S2) site of hSERT with minimal conformational change from its solid-state structure, stabilized by multiple key interactions including a salt bridge, pi-stacking, and pi-cation interactions[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel albino rats (70-90 days old, 200-250 g, behavioral despair induced via Porsolt forced swimming test)[2]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; single dose
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Result:Significantly shortened the duration of immobility (depressive state) compared to control.
Chemical Information
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CAS No. 63302-99-8
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Appearance Solid
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Molecular Weight 388.29
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Formula C16H23Cl2N5O2
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Color Light yellow to green yellow
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SMILES
[H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3.O
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Synonyms
Azafen monohydrate; Pipofezin dihydrochloride monohydrate; Pipofezine dihydrochloride monohydrate
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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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochim Biophys Acta Gen Subj
5-Hydroxytryptamine activates a 5-HT/c-Myc/SLC6A4 signaling loop in non-small cell lung cancer. [Abstract]2022 Apr;1866(4):130093. PMID: 35066124
Solvent & Solubility
In Vitro:
H2O : ≥ 100 mg/mL (257.54 mM)
DMSO : 1 mg/mL (2.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (128.77 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (287 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)
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). 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 / H2O | 1 mM | 2.5754 mL | 12.8770 mL | 25.7539 mL | 64.3849 mL |
| H2O | 5 mM | 0.5151 mL | 2.5754 mL | 5.1508 mL | 12.8770 mL |
| 10 mM | 0.2575 mL | 1.2877 mL | 2.5754 mL | 6.4385 mL | |
| 15 mM | 0.1717 mL | 0.8585 mL | 1.7169 mL | 4.2923 mL | |
| 20 mM | 0.1288 mL | 0.6438 mL | 1.2877 mL | 3.2192 mL | |
| 25 mM | 0.1030 mL | 0.5151 mL | 1.0302 mL | 2.5754 mL | |
| 30 mM | 0.0858 mL | 0.4292 mL | 0.8585 mL | 2.1462 mL | |
| 40 mM | 0.0644 mL | 0.3219 mL | 0.6438 mL | 1.6096 mL | |
| 50 mM | 0.0515 mL | 0.2575 mL | 0.5151 mL | 1.2877 mL | |
| 60 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.0731 mL | |
| 80 mM | 0.0322 mL | 0.1610 mL | 0.3219 mL | 0.8048 mL | |
| 100 mM | 0.0258 mL | 0.1288 mL | 0.2575 mL | 0.6438 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Azaphen dihydrochloride monohydrate Related Classifications
HY-A0022A Related Classifications
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Keywords
- Azaphen dihydrochloride
- 63302-99-8
- Azafen
- Pipofezin dihydrochloride
- Pipofezine dihydrochloride
- Serotonin Transporter
- 5-HT Receptor
- human serotonin transporter
- hSERT
- monoamine reuptake
- muscarinic receptors
- serotonin
- depression
- 5-HT2c receptors
- Normura forced swimming test
- Porsolt behavioral despair test
- monoamine oxidase
- Inhibitor
- inhibitor
- inhibit