DuP 734
Based on 1 Customer Validation
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.
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- Reinheit: 98.82%
- CAS. Nr.: 135135-87-4
- Formel: C17H23BrFNO
- Molecular Weight:356.27
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Speicherung:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biologische Aktivität
Administration of DuP 734 potently antagonizes the binding of [3H]DuP 734 and [3H](+)-SKF 10,047 to brain sigma receptors in vivo with ID50 values of 0.02 and 0.07 mg/kg (0.07 and 0.25μmol/kg), respectively[2].
Following intravenous dosing, the disposition of DuP 734 in mice, rats, beagle dogs and cynomolgus monkeys is characterized by high total body systemic plasma clearance (46 to 87 mL/min/kg) and large steady-state volume of distribution (3.6 to 6.8 L/kg). The terminal elimination half-life ranged from 50 to 83 min. The gastrointestinal absorption from an aqueous solution is very rapid in mice and rats with peak DuP 734 plasma concentrations attain within 5 and 20 min following administration, respectively. The peak plasma concentrations in dogs and monkeys are attained within 45 and 130 min, respectively. The absolute bioavailability in mice ranges from 29 to 46% at doses of 3.1 to 30.1 mg/kg. The bioavailability increases from 4 to 10% and from 14 to 72% when doses are increased from 12.5 to 50 mg/kg and 1 to 3 mg/kg of DuP 734 in rats and dogs, respectively. The bioavailability in monkeys is 30.5% at 9.3 mg/kg DuP 734 dose. The dose dependent pharmacokinetics of DuP 734 is observed within narrow dose ranges in all animal species investigated[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 135135-87-4
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Appearance Solid
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Molecular Weight 356.27
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Formel C17H23BrFNO
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Color Off-white to light yellow
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SMILES
FC1=CC=C(C(CC2CCN(CC3CC3)CC2)=O)C=C1.[H]Br
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (701.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (280.69 mM)
* "≥" 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 (stored under nitrogen, 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 (stored under nitrogen, 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. L Cook, et al. DuP 734 [1-(cyclopropylmethyl)-4-(2'(4''-fluorophenyl)-2'- Oxoethyl)piperidine HBr], a Potential Antipsychotic Agent: Preclinical Behavioral Effects. J Pharmacol Exp Ther. 1992 Dec;263(3):1159-66. [Content Brief]
[2]. M Watanabe, et al. [3H]1-(cyclopropylmethyl)-4-(2-(4-fluorophenyl)-2-oxoethyl) Piperidine HBr (DuP 734). A Selective Ligand for Sigma Receptors in Mouse Brain in Vivo. J Pharmacol Exp Ther. 1993 Sep;266(3):1541-8. [Content Brief]
[3]. R P Kapil, et al. Dose and Species Dependent Pharmacokinetics of a Novel Sigma Receptor Antagonist, DuP 734. Res Commun Mol Pathol Pharmacol. 1995 Apr;88(1):3-20. [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 (stored under nitrogen, 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.8069 mL | 14.0343 mL | 28.0686 mL | 70.1715 mL |
| 5 mM | 0.5614 mL | 2.8069 mL | 5.6137 mL | 14.0343 mL | |
| 10 mM | 0.2807 mL | 1.4034 mL | 2.8069 mL | 7.0172 mL | |
| 15 mM | 0.1871 mL | 0.9356 mL | 1.8712 mL | 4.6781 mL | |
| 20 mM | 0.1403 mL | 0.7017 mL | 1.4034 mL | 3.5086 mL | |
| 25 mM | 0.1123 mL | 0.5614 mL | 1.1227 mL | 2.8069 mL | |
| 30 mM | 0.0936 mL | 0.4678 mL | 0.9356 mL | 2.3391 mL | |
| 40 mM | 0.0702 mL | 0.3509 mL | 0.7017 mL | 1.7543 mL | |
| 50 mM | 0.0561 mL | 0.2807 mL | 0.5614 mL | 1.4034 mL | |
| 60 mM | 0.0468 mL | 0.2339 mL | 0.4678 mL | 1.1695 mL | |
| 80 mM | 0.0351 mL | 0.1754 mL | 0.3509 mL | 0.8771 mL | |
| 100 mM | 0.0281 mL | 0.1403 mL | 0.2807 mL | 0.7017 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.
DuP 734 Related Classifications
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