Eplivanserin hemifumarate |
| Catalog No.GC50084 |
El hemifumarato de eplivanserina (SR-46349) es un antagonista del receptor 5-HT2A potente, selectivo y activo por vÍa oral, con una IC50 de 5,8 nM en la membrana cortical de rata y una Kd de 1,14 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130580-02-8
Sample solution is provided at 25 µL, 10mM.
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Potent and selective 5-HT2A antagonist (IC50 values are 5.8 and 120 and >100 nM for 5-HT2A, 5-HT2B and 5-HT2C, respectively). Attenuates cocaine-induced hyperactivity. Increases dopamine (DA) release in rat medial prefrontal cortex (mPFC); potentiates haloperidol-induced DA release in the mPFC and nucleus accumbens.
Yadav et al (2011) Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. J.Pharmacol.Exp.Ther. 339 99 PMID:21737536 |Filip et al (2004) Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. J.Pharmacol.Exp.Ther. 310 1246 PMID:15131246 |Bonaccorso et al (2002) SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced DA release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 27 430 PMID:12225700
| Cas No. | 130580-02-8 | SDF | |
| Canonical SMILES | OC(C=C2)=CC=C2/C=C/C(C1=CC=CC=C1F)=N/OCCN(C)C.O=C(/C=C/C(O)=O)O.OC(C=C4)=CC=C4/C=C/C(C3=CC=CC=C3F)=N/OCCN(C)C | ||
| Formula | C19H21FN2O2.0.5C4H4O4 | M.Wt | 386.42 |
| Solubility | Soluble 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5879 mL | 12.9393 mL | 25.8786 mL |
| 5 mM | 0.5176 mL | 2.5879 mL | 5.1757 mL |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5879 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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