Pipamperone
Based on 1 Customer Validation
Pipamperone (Floropipamide) is a butyrophenone derivative and high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0). Pipamperone is also a low-affinity antagonist of D2 receptor (pKi=6.7). Pipamperone affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease.
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- Pureté: 99.89%
- CAS No.: 1893-33-0
- Formule: C21H30FN3O2
- Masse moléculaire:375.48
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
5-HT2A Receptor 8.2 (pKi) |
D4 Receptor 8.0 (pKi) |
D2 Receptor 6.7 (pKi) |
5-HT2A Receptor |
5-HT2C Receptor 6.9 (pKi) |
5-HT1 Receptor 5.7 (pKi) |
α1 receptor 7.2 (pKi) |
In Vitro
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1893-33-0
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Appearance Solid
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Masse moléculaire 375.48
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Formule C21H30FN3O2
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Color White to off-white
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SMILES
O=C(C1(N2CCCCC2)CCN(CCCC(C3=CC=C(F)C=C3)=O)CC1)N
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Synonyms
Floropipamide; McN-JR 3345; R 3345
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (266.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 25 mg/mL (66.58 mM; Need ultrasonic)
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 (protect from light). 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 (protect from light). 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)
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 (6.66 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 (6.66 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Oekelen DV, et al. Different regulation of rat 5-HT(2A) and rat 5-HT(2C) receptors in NIH 3T3 cells upon exposure to 5-HT and pipamperone. Eur J Pharmacol. 2001 Aug 3;425(1):21-32. [Content Brief]
[4]. Kamp D, et al. Hypothermia in a patient with Alzheimer's disease receiving a combination therapy with risperidone and pipamperone. Ther Adv Psychopharmacol. 2016 Feb;6(1):55-7. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| 0.1 M HCl / DMSO | 1 mM | 2.6633 mL | 13.3163 mL | 26.6326 mL | 66.5814 mL |
| 5 mM | 0.5327 mL | 2.6633 mL | 5.3265 mL | 13.3163 mL | |
| 10 mM | 0.2663 mL | 1.3316 mL | 2.6633 mL | 6.6581 mL | |
| 15 mM | 0.1776 mL | 0.8878 mL | 1.7755 mL | 4.4388 mL | |
| 20 mM | 0.1332 mL | 0.6658 mL | 1.3316 mL | 3.3291 mL | |
| 25 mM | 0.1065 mL | 0.5327 mL | 1.0653 mL | 2.6633 mL | |
| 30 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2194 mL | |
| 40 mM | 0.0666 mL | 0.3329 mL | 0.6658 mL | 1.6645 mL | |
| 50 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3316 mL | |
| 60 mM | 0.0444 mL | 0.2219 mL | 0.4439 mL | 1.1097 mL | |
| DMSO | 80 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6658 mL |
Pipamperone Related Classifications
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