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| 5mg |
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| 10mg |
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| Targets |
Xaliproden targets the serotonin 5-HT1A receptor. As a full agonist of the 5-HT1A receptor, it activates the receptor, modulating serotonergic neurotransmission. It also mimics the effects of nerve growth factor (NGF), suggesting it may have neurotrophic effects.
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| ln Vitro |
Xaliproden is a potent and selective 5-HT1A receptor agonist with an IC50 of 3 nM in a radioligand binding assay. It exhibits anti-depression and anti-anxiety effects. It may possess therapeutic potential for the research of neurodegenerative diseases.
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| ln Vivo |
Specific in vivo activity data for xaliproden is not extensively detailed in the available literature. As a 5-HT1A receptor agonist with NGF-like effects, it has been studied for potential therapeutic applications in neurodegenerative diseases. Further studies are needed to fully characterize its in vivo efficacy.
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| Enzyme Assay |
Xaliproden's affinity for the 5-HT1A receptor is assessed using in vitro radioligand binding assays. These assays measure the compound's ability to displace a radiolabeled ligand from the receptor. The IC50 of 3 nM is determined from competition binding curves.
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| Cell Assay |
Cellular assays for xaliproden involve treating cells expressing the 5-HT1A receptor with the compound and measuring receptor activation. Functional assays, such as GTPγS binding or cAMP accumulation, are used to assess agonist activity. Its NGF-like effects can be evaluated in neuronal cell cultures.
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| Animal Protocol |
In vivo animal model protocols for xaliproden would involve its administration to animal models of depression, anxiety, or neurodegenerative diseases. Its effects on behavior, neuroprotection, and neurotransmitter levels would be assessed.
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| ADME/Pharmacokinetics |
Xaliproden hydrochloride has a molecular weight of 417.89 and a molecular formula of C24H22F3N·HCl. It is soluble in DMSO (≥5 mg/mL). Specific pharmacokinetic data is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of xaliproden has not been extensively characterized in the available literature. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References |
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| Additional Infomation |
Xaliproden hydrochloride belongs to the naphthalene family of compounds. Xaliproden hydrochloride is the hydrochloride salt of Xaliproden, an orally potent synthetic non-peptide serotonin (5-HT) 1A receptor agonist with neurotrophic and neuroprotective effects. Although its mechanism of action is not fully elucidated, Xaliproden appears to mimic the effects of neurotrophic factors or stimulate their synthesis, thereby promoting neuronal differentiation and proliferation and inhibiting neuronal death. The neuroprotective effect of this drug involves activating the MAP kinase pathway by stimulating the 5-HT1A receptor. See also: Xaliproden (note moved to).
Xaliproden hydrochloride (CAS# 90494-79-4) is a research compound used to study the 5-HT1A receptor and its role in depression, anxiety, and neurodegenerative diseases. It is a potent and selective 5-HT1A receptor agonist that also mimics NGF effects. It is not approved for clinical use. |
| Molecular Formula |
C24H22NF3.HCL
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|---|---|
| Molecular Weight |
417.89432
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| Exact Mass |
417.147
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| CAS # |
90494-79-4
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| Related CAS # |
90494-79-4 (HCl);135354-02-8;
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| PubChem CID |
128918
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| Appearance |
White to off-white solid powder
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| Boiling Point |
487.8ºC at 760mmHg
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| Flash Point |
248.8ºC
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| LogP |
6.93
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WVHBEIJGAINUBW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H22F3N.ClH/c25-24(26,27)23-7-3-6-22(17-23)20-11-14-28(15-12-20)13-10-18-8-9-19-4-1-2-5-21(19)16-18;/h1-9,11,16-17H,10,12-15H2;1H
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| Chemical Name |
1-(2-naphthalen-2-ylethyl)-4-[3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-pyridine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~79.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3930 mL | 11.9649 mL | 23.9297 mL | |
| 5 mM | 0.4786 mL | 2.3930 mL | 4.7859 mL | |
| 10 mM | 0.2393 mL | 1.1965 mL | 2.3930 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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