Pramocaine hydrochloride
Based on 1 Customer Validation
Pramocaine (Pramoxine) hydrochloride is a topical surface anesthetic and antipruritic agent. Pramocaine hydrochloride reversibly inhibits voltage-gated sodium channel, reduces transmembrane permeability of sodium ions, stabilizes cell membranes, prevents depolarization, blocks action potential conduction, and inhibits peripheral slow C-fiber pathways associated with pain, pruritus and thermoception. Pramocaine hydrochloride can be used in research related to chronic pruritus, renal pruritus, atopic dermatitis, xerotic pruritus, uremic pruritus, and cutaneous hyperalgesia/pain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.85%
- CAS. Nr.: 637-58-1
- Formel: C17H28ClNO3
- Molecular Weight:329.86
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vivo
Pramocaine (7.74-30.96 μmol/kg; intrathecal; single injection) hydrochloride produces dose-dependent spinal sensory and motor block in rats, with ED50 values ranging from 15.47 to 17.77 μmol/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 298 to 348 g)[2]
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Dosage:7.74 μmol/kg; 15.48 μmol/kg; 23.22 μmol/kg; 30.96 μmol/kg
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Administration:intrathecal; single injection
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Result:Elicited dose-dependent spinal block of nociception, proprioception, and motor function.
Determined ED50 values of 15.47 μmol/kg for nociceptive block, 16.46 μmol/kg for proprioceptive block, and 17.77 μmol/kg for motor block.
Reported mean ED75 and ED25 values across all three block types as 20.83 μmol/kg and 13.17 μmol/kg, respectively.
Produced 100% maximum possible effect (%MPE) for all three block types at 30.96 μmol/kg, with complete blockade times of 36.9 minutes for nociception, 17.8 minutes for proprioception, and 15.4 minutes for motor function.
Recorded full recovery times of 94.2 minutes for nociception, 65.6 minutes for proprioception, and 41.3 minutes for motor function at 30.96 μmol/kg.
Measured AUC values of 6425 (%MPE × min) for nociception, 3709 (%MPE × min) for proprioception, and 2362 (%MPE × min) for motor function at 30.96 μmol/kg.
Showed no significant difference in spinal block duration compared to bupivacaine at equipotent doses (ED75, ED50, ED25).
Chemical Information
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CAS. Nr. 637-58-1
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Appearance Solid
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Molecular Weight 329.86
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Formel C17H28ClNO3
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Color White to off-white
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SMILES
CCCCOC1=CC=C(OCCCN2CCOCC2)C=C1.[H]Cl
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Synonyms
Pramoxine hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (303.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (303.16 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (7.58 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 (7.58 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (303.16 mM); Clear solution; Need ultrasonic
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.
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 (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1].
Agarwal A, et al. Topical Pramoxine in Chronic Pruritus: Where do We Stand? Indian J Dermatol. 2021 Sep-Oct;66(5):576.
[Content Brief]
[2]. Chou AK, et al. Intrathecal pramoxine causes long-lasting spinal sensory and motor block in rats. The Journal of pharmacy and pharmacology. 2018 Apr;70(4):543-549. [Content Brief]
[3]. Chou AK, et al. Skin nociceptive block with pramoxine delivery by subcutaneous injection in rats. Pharmacological reports : PR. 2018 Dec;70(6):1180-1184. [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 (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 |
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| DMSO / H2O | 1 mM | 3.0316 mL | 15.1579 mL | 30.3159 mL | 75.7897 mL |
| 5 mM | 0.6063 mL | 3.0316 mL | 6.0632 mL | 15.1579 mL | |
| 10 mM | 0.3032 mL | 1.5158 mL | 3.0316 mL | 7.5790 mL | |
| 15 mM | 0.2021 mL | 1.0105 mL | 2.0211 mL | 5.0526 mL | |
| 20 mM | 0.1516 mL | 0.7579 mL | 1.5158 mL | 3.7895 mL | |
| 25 mM | 0.1213 mL | 0.6063 mL | 1.2126 mL | 3.0316 mL | |
| 30 mM | 0.1011 mL | 0.5053 mL | 1.0105 mL | 2.5263 mL | |
| 40 mM | 0.0758 mL | 0.3789 mL | 0.7579 mL | 1.8947 mL | |
| 50 mM | 0.0606 mL | 0.3032 mL | 0.6063 mL | 1.5158 mL | |
| 60 mM | 0.0505 mL | 0.2526 mL | 0.5053 mL | 1.2632 mL | |
| 80 mM | 0.0379 mL | 0.1895 mL | 0.3789 mL | 0.9474 mL | |
| 100 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL | 0.7579 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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