EST73502 monohydrochloride
Based on 1 Customer Validation
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.
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- Purity: 99.58%
- CAS No.: 2535970-65-9
- 화학식: C19H27ClF2N2O2
- 분자량:388.88
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
Ki: 64 nM (MOR), 118 nM (σ1R)[1]
EST73502 monohydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 mice, PSNL model[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection, twice a day, for 10 days
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Result:Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.
Chemical Information
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CAS No. 2535970-65-9
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Appearance Solid
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분자량 388.88
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화학식 C19H27ClF2N2O2
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Color White to off-white
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SMILES
FC1=CC=C(F)C=C1CCN(CC2)CCC2(O[C@@H]3C)CN(CC)C3=O.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 50 mg/mL (128.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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: ≥ 2.5 mg/mL (6.43 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 (6.43 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.
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.
순도&문서
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Data Sheet (273 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)
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5715 mL | 12.8574 mL | 25.7149 mL | 64.2872 mL |
| 5 mM | 0.5143 mL | 2.5715 mL | 5.1430 mL | 12.8574 mL | |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5715 mL | 6.4287 mL | |
| 15 mM | 0.1714 mL | 0.8572 mL | 1.7143 mL | 4.2858 mL | |
| 20 mM | 0.1286 mL | 0.6429 mL | 1.2857 mL | 3.2144 mL | |
| 25 mM | 0.1029 mL | 0.5143 mL | 1.0286 mL | 2.5715 mL | |
| 30 mM | 0.0857 mL | 0.4286 mL | 0.8572 mL | 2.1429 mL | |
| 40 mM | 0.0643 mL | 0.3214 mL | 0.6429 mL | 1.6072 mL | |
| 50 mM | 0.0514 mL | 0.2571 mL | 0.5143 mL | 1.2857 mL | |
| 60 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0715 mL | |
| 80 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8036 mL | |
| 100 mM | 0.0257 mL | 0.1286 mL | 0.2571 mL | 0.6429 mL |
EST73502 monohydrochloride Related Classifications
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