2. Neuronal Signaling
  3. Sigma Receptor
  4. DuP 734

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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DuP 734 Chemical Structure

DuP 734 Chemical Structure

CAS No. : 135135-87-4

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10 mM * 1 mL in DMSO
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Description

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[1][2][3].

IC50 & Target

Sigma receptor; 5-HT2 receptor; D2 receptor[1][2][3]
In Vivo

DuP 734 potently blocks mescaline-induced scratching (ED50=0.35 mg/kg, p.o.) and aggressive activity (ED50=1.9 mg/kg, p.o.) and is relatively much weaker as an apomorphine antagonist (ED50=12 mg/kg, p.o.)[1].
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.
Molecular Weight

356.27

Formula

C17H23BrFNO
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC=C(C(CC2CCN(CC3CC3)CC2)=O)C=C1.[H]Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8069 mL 14.0343 mL 28.0686 mL
5 mM 0.5614 mL 2.8069 mL 5.6137 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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 (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.

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DuP 734 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DuP 734135135-87-4DuP734DuP-734Sigma Receptorsigma5-HT2antipsychoticInhibitorinhibitorinhibit

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