S1RA [878141-96-9]
Cat# HY-18099-5mg
Size : 5mg
Marca : MedChemExpress
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice.
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S1RA Chemical Structure
CAS No. : 878141-96-9
This product is a controlled substance and not for sale in your territory.
Based on 1 publication(s) in Google Scholar
Other Forms of S1RA:
- S1RA hydrochloride In-stock
Description |
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice[1][2]. |
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IC50 & Target[1][3] |
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In Vitro |
S1RA (E-52862; 100 µM; 4 h) inhibit intracellular calcium responses in TRPA1 expressing HEK293 cells[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
S1RA (E-52862; 40 mg/kg; IP; single dose) produces a substantial reduction in pain-related responses to intradermal Allylisothiocyanate (AITC) in WT mice[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Masse moléculaire |
337.42 |
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Formule |
C20H23N3O2 |
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CAS No. |
878141-96-9 |
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Appearance |
Solid |
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Color |
Off-white to yellow |
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SMILES |
CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3 |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
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Solvant et solubilité |
In Vitro:
1M HCl : 50 mg/mL (148.18 mM; ultrasonic and adjust pH to 1 with HCl) DMSO : 33.33 mg/mL (98.78 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) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
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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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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Pureté et documentation | |||||||||||||
Références |
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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 / 1M HCl | 1 mM | 2.9637 mL | 14.8183 mL | 29.6367 mL | 74.0916 mL |
5 mM | 0.5927 mL | 2.9637 mL | 5.9273 mL | 14.8183 mL | |
10 mM | 0.2964 mL | 1.4818 mL | 2.9637 mL | 7.4092 mL | |
15 mM | 0.1976 mL | 0.9879 mL | 1.9758 mL | 4.9394 mL | |
20 mM | 0.1482 mL | 0.7409 mL | 1.4818 mL | 3.7046 mL | |
25 mM | 0.1185 mL | 0.5927 mL | 1.1855 mL | 2.9637 mL | |
30 mM | 0.0988 mL | 0.4939 mL | 0.9879 mL | 2.4697 mL | |
40 mM | 0.0741 mL | 0.3705 mL | 0.7409 mL | 1.8523 mL | |
50 mM | 0.0593 mL | 0.2964 mL | 0.5927 mL | 1.4818 mL | |
60 mM | 0.0494 mL | 0.2470 mL | 0.4939 mL | 1.2349 mL | |
80 mM | 0.0370 mL | 0.1852 mL | 0.3705 mL | 0.9261 mL | |
1M HCl | 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7409 mL |