Oxypertine
Based on 1 Customer Validation
Oxypertine (WIN-18501-2) is a neuroprotective agent. Oxypertine shows high affinity for the 5-HT2 and dopamine D2 receptors with Kis of 8.6 nM and 30 nM, respectively. Oxypertine can be used in the research of neurological conditions, such as anxiety and schizophrenia.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 153-87-7
- Formula: C23H29N3O2
- Molecular Weight:379.50
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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D2 Receptor 30 nM (Ki) |
5-HT2 Receptor 8.6 nM (Ki) |
Oxypertine (0.44 nM-26 μM, 15 min) antagonizes dopamine and 5-HT induced contractions of the rat isolated vas deferens[1].
Oxypertine (8.8 nM, 15 min) reduces the contractions evoked by transmural stimulation of the vas deferens[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Oxypertine (0.625-20 mg/kg, i.p.) inhibits stereotyped behaviour induced by both amphetamine and apomorphine in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with chronic restraint stress[2]
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Dosage:10, 35 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Increased the level of homovanillic acid in three discrete regions, i.e., the cortex, striatum and mid-brain.
Inhibited Apomorphine-induced stereotypy.
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Animal Model:Mice with stereotyped behaviour induced by amphetamine (5.0 mg/kg i.p.) and apomorphine (1.0 mg/kg, s.c.)[3]
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Dosage:0.625-20 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced the content of dopamine in the striatum but increased the concentrations of homovanillic acid (HVA) and 3,4-dihydroxyphenylacetic acid (DOPAC).
Chemical Information
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CAS No. 153-87-7
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Appearance Solid
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Molecular Weight 379.50
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Formula C23H29N3O2
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Color Off-white to light brown
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SMILES
CC(NC1=C2C=C(OC)C(OC)=C1)=C2CCN3CCN(CC3)C4=CC=CC=C4
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Synonyms
WIN-18501-2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (263.50 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.59 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 (6.59 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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. H Miranda, et al. Effects of oxypertine on the isolated vas deferens of the rat. Br J Pharmacol. 1978 Apr;62(4):515-8. [Content Brief]
[2]. T Moroji, et al. Neurochemical and behavioral studies on the mode of action of oxypertine. Arzneimittelforschung. 1986 May;36(5):804-8. [Content Brief]
[3]. M Hong, et al. Comparison of the acute actions of amine-depleting drugs and dopamine receptor antagonists on dopamine function in the brain in rats. [Content Brief]
[4]. Megens AA, et al. Risperidone and related 5HT2/D2 antagonists: a new type of antipsychotic agent? Prog Med Chem. 1996;33:185-232. [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, 6 months; -20°C, 1 month. 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 | 2.6350 mL | 13.1752 mL | 26.3505 mL | 65.8762 mL |
| 5 mM | 0.5270 mL | 2.6350 mL | 5.2701 mL | 13.1752 mL | |
| 10 mM | 0.2635 mL | 1.3175 mL | 2.6350 mL | 6.5876 mL | |
| 15 mM | 0.1757 mL | 0.8783 mL | 1.7567 mL | 4.3917 mL | |
| 20 mM | 0.1318 mL | 0.6588 mL | 1.3175 mL | 3.2938 mL | |
| 25 mM | 0.1054 mL | 0.5270 mL | 1.0540 mL | 2.6350 mL | |
| 30 mM | 0.0878 mL | 0.4392 mL | 0.8783 mL | 2.1959 mL | |
| 40 mM | 0.0659 mL | 0.3294 mL | 0.6588 mL | 1.6469 mL | |
| 50 mM | 0.0527 mL | 0.2635 mL | 0.5270 mL | 1.3175 mL | |
| 60 mM | 0.0439 mL | 0.2196 mL | 0.4392 mL | 1.0979 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3294 mL | 0.8235 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2635 mL | 0.6588 mL |