2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Eplivanserin hemifumarate

Eplivanserin hemifumarate  (Synonyms: SR-46349 hemifumarate; SR 46349B)

Cat. No.: HY-110129 Purity: 98.07%
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Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.

For research use only. We do not sell to patients.

Eplivanserin hemifumarate Chemical Structure

Eplivanserin hemifumarate Chemical Structure

CAS No. : 130580-02-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Eplivanserin hemifumarate:

Eplivanserin hemifumarate Related Antibodies

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Description

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].

IC50 & Target[1][2]

5-HT2A Receptor

5.8 nM (IC50)

5-HT2C Receptor

120 nM (IC50)

In Vitro

Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D). Eplivanserin also has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na+ channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Eplivanserin hemifumarate Related Antibodies
In Vivo

Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice[1].
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

386.43

Formula

C19H21FN2O2.1/2C4H4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)/C=C/C(O)=O.OC(C=C1)=CC=C1/C=C/C(C2=C(C=CC=C2)F)=N/OCCN(C)C.[1/2]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.69 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
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5878 mL 12.9390 mL 25.8779 mL
5 mM 0.5176 mL 2.5878 mL 5.1756 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.07%

COA (251 KB) RP-HPLC (239 KB)

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 2.5878 mL 12.9390 mL 25.8779 mL 64.6948 mL
5 mM 0.5176 mL 2.5878 mL 5.1756 mL 12.9390 mL
10 mM 0.2588 mL 1.2939 mL 2.5878 mL 6.4695 mL
15 mM 0.1725 mL 0.8626 mL 1.7252 mL 4.3130 mL
20 mM 0.1294 mL 0.6469 mL 1.2939 mL 3.2347 mL
25 mM 0.1035 mL 0.5176 mL 1.0351 mL 2.5878 mL
30 mM 0.0863 mL 0.4313 mL 0.8626 mL 2.1565 mL
40 mM 0.0647 mL 0.3235 mL 0.6469 mL 1.6174 mL
50 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2939 mL
60 mM 0.0431 mL 0.2156 mL 0.4313 mL 1.0782 mL
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Eplivanserin hemifumarate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eplivanserin hemifumarate130580-02-8SR-46349 hemifumarate SR 46349B5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2AoraldopaminereleaseInhibitorinhibitorinhibit

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