PRX-07034 hydrochloride
Based on 1 Customer Validation
PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.
For research use only. We do not sell to patients.
- Purity: 98.97%
- CAS No.: 903580-39-2
- Formula: C21H29Cl2N3O4S
- Molecular Weight:490.44
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT6 Receptor 4-8 nM (Ki) |
5-HT6 Receptor |
5-HT6 Receptor 19 nM (IC50) |
5-HT1B Receptor 260 nM (Ki) |
5-HT1A Receptor 420 nM (Ki) |
5-HT1D Receptor 2.8 μM (Ki) |
5-HT2A Receptor 2.5 μM (IC50) |
5-HT2B Receptor 2.5 μM (IC50) |
5-HT2C Receptor 3.7 μM (IC50) |
Dopamine D3 Receptor 71 nM (Ki) |
Opioid μ Receptor 0.45 μM (Ki) |
Histamine H2 Receptor 0.64 μM (Ki) |
PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 μM, 71 nM, 0.64 μM, and 0.45 μM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 μM, 2.5 μM, and 3.7 μM, respectively[1].
In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50=4.8 μM) and very low agonistic activity for the opioid μ-receptor (EC50=19 μM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Long-Evans rats weighing approximately 350 g[1]
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Dosage:0.1, 1, or 3 mg/kg
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Administration:Injected intraperitoneal
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Result:1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination.
Chemical Information
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CAS No. 903580-39-2
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Appearance Solid
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Molecular Weight 490.44
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Formula C21H29Cl2N3O4S
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Color White to off-white
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SMILES
O=S(C1=CC=C(N2CCNCC2)C=C1NC(C)C3=CC(Cl)=CC(OC)=C3OC)(C)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 31.25 mg/mL (63.72 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.76 mg/mL (9.71 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 (sealed storage, 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 (sealed storage, 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.
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: ≥ 2.08 mg/mL (4.24 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 (4.24 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.
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 (sealed storage, away from moisture)
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 (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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 (sealed storage, 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 | 2.0390 mL | 10.1949 mL | 20.3899 mL | 50.9746 mL |
| 5 mM | 0.4078 mL | 2.0390 mL | 4.0780 mL | 10.1949 mL | |
| DMSO | 10 mM | 0.2039 mL | 1.0195 mL | 2.0390 mL | 5.0975 mL |
| 15 mM | 0.1359 mL | 0.6797 mL | 1.3593 mL | 3.3983 mL | |
| 20 mM | 0.1019 mL | 0.5097 mL | 1.0195 mL | 2.5487 mL | |
| 25 mM | 0.0816 mL | 0.4078 mL | 0.8156 mL | 2.0390 mL | |
| 30 mM | 0.0680 mL | 0.3398 mL | 0.6797 mL | 1.6992 mL | |
| 40 mM | 0.0510 mL | 0.2549 mL | 0.5097 mL | 1.2744 mL | |
| 50 mM | 0.0408 mL | 0.2039 mL | 0.4078 mL | 1.0195 mL | |
| 60 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8496 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.
PRX-07034 hydrochloride Related Classifications
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