S1RA (Synonyms: E-52862) |
| رقم الكتالوجGC10407 |
S1RA (E-52862) هو مستقبل سيجما -1 قوي وانتقائي (σ1R ، Ki = 17 نانومتر) ، أظهر انتقائية جيدة ضد σ2R (Ki> 1000 نانومتر)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 878141-96-9
Sample solution is provided at 25 µL, 10mM.
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S1RA is a potent and selective antagonist of σ1 receptor (σ1R) with Ki value of 17nM [1].
S1RA is the first σ1 receptor antagonist with potent antinociceptive activities in various pain models. In the binding assay, S1RA shows good affinity to human σ1 receptor transfected in HEK293 membranes with Ki value of 17nM. The Ki value for guinea pig brain membrane σ1 receptor is higher than 1μM. S1RA also shows no significant affinity to another 170 molecular targets including receptors, ion channels and enzymes [1, 2].
In the mouse tests, S1RA exhibits potent analgesic effects on capsaicin-induced mechanical hypersensitivity and formalin-induced pain. Besides that, S1RA inhibits both mechanical allodynia and thermal hypersensitivity with ED50 values of 23.4mg/kg and 18.8mg/kg in the partial sciatic nerve ligation model in mice [1].
References:
[1] Díaz J L, Cuberes R, Berrocal J, et al. Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1 H-pyrazol-3-yloxy] ethyl} morpholine (S1RA, E-52862). Journal of medicinal chemistry, 2012, 55(19): 8211-8224.
[2] Wunsch B. The σ1 Receptor Antagonist S1RA Is a Promising Candidate for the Treatment of Neurogenic PainJ. Journal of medicinal chemistry, 2012, 55(19): 8209-8210.
| Cas No. | 878141-96-9 | SDF | |
| المرادفات | E-52862 | ||
| Chemical Name | 4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine | ||
| Canonical SMILES | CC1=CC(OCCN2CCOCC2)=NN1C3=CC4=CC=CC=C4C=C3 | ||
| Formula | C20H23N3O2 | M.Wt | 337.42 |
| الذوبان | ≥ 10.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9637 mL | 14.8183 mL | 29.6367 mL |
| 5 mM | 592.7 μL | 2.9637 mL | 5.9273 mL |
| 10 mM | 296.4 μL | 1.4818 mL | 2.9637 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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