E1R
Based on 1 Customer Validation
E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.83%
- No. CAS: 1301211-78-8
- Fòrmula: C13H16N2O2
- Peso molecular:232.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Sigma Receptor
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Actividad biológica
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Sigma 1 Receptor |
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Cell Line
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Type | Value | Description | References |
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| Jurkat | IC50 |
43 nM
Compound: E1R, 4R,5S-2a
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Displacement of [3H]1,3-di(2-tolyl)guanidine from sigma 1 receptor in human Jurkat cells
Displacement of [3H]1,3-di(2-tolyl)guanidine from sigma 1 receptor in human Jurkat cells
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[PMID: 23582449] |
The only target for E1R (inhibition or enhancement of radioligand binding exceeding 20%) is the sigma receptor. 10 μM E1R does not displace the radioligand, but instead increases the specific binding of a non-selective radioligand ([3H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells[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 ICR and Balb/c mice weighed 23-25 g[1]
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Dosage:0.1, 1 and 10 mg/kg
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Administration:Administered i.p. 60 min before the training session
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Result:Treatment at doses of 1 and 10 mg/kg increased retention latency by 194 and 211%, respectively, compared with the control group.
Chemical Information
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No. CAS 1301211-78-8
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Appearance Solid
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Peso molecular 232.28
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Fòrmula C13H16N2O2
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Color Off-white to yellow
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SMILES
O=C(CN1C(C[C@@H]([C@@H]1C)C2=CC=CC=C2)=O)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (430.51 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. 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. 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: ≥ 5 mg/mL (21.53 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (21.53 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (43.05 mM); Clear solution; Need ultrasonic
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.
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 1 mM | 4.3051 mL | 21.5255 mL | 43.0509 mL | 107.6273 mL |
| 5 mM | 0.8610 mL | 4.3051 mL | 8.6102 mL | 21.5255 mL | |
| 10 mM | 0.4305 mL | 2.1525 mL | 4.3051 mL | 10.7627 mL | |
| 15 mM | 0.2870 mL | 1.4350 mL | 2.8701 mL | 7.1752 mL | |
| 20 mM | 0.2153 mL | 1.0763 mL | 2.1525 mL | 5.3814 mL | |
| 25 mM | 0.1722 mL | 0.8610 mL | 1.7220 mL | 4.3051 mL | |
| 30 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5876 mL | |
| 40 mM | 0.1076 mL | 0.5381 mL | 1.0763 mL | 2.6907 mL | |
| 50 mM | 0.0861 mL | 0.4305 mL | 0.8610 mL | 2.1525 mL | |
| 60 mM | 0.0718 mL | 0.3588 mL | 0.7175 mL | 1.7938 mL | |
| 80 mM | 0.0538 mL | 0.2691 mL | 0.5381 mL | 1.3453 mL | |
| 100 mM | 0.0431 mL | 0.2153 mL | 0.4305 mL | 1.0763 mL |
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