1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SR 57227A

5-HT3 receptor

SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

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

SR 57227A Chemical Structure

SR 57227A Chemical Structure

CAS No. : 77145-61-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 154 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects[1][2].

In Vitro

SR 57227A binds to 5-HT3 receptors labelled with [3H]S-zacopride with an affinity (Ki) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes and 103 nM in whole NG 108-15 cell[1].

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

In Vivo

SR 57227A (1-30 mg/kg; i.p.) dose-dependently reduces immobility time in the forced swimming test with an ED50 value for this effect of 14.2 mg/kg[2].
In the forced swimming test, SR 57227A dose-dependently reduces the duration of immobility in rats after i.p. administration. (ED50=7.6 mg/kg i.p. in rats.) SR 57227A is also active in both species after oral administration. In a time-course study in mice, SR 57227A (20 mg/kg p.o.) produces a significant effect lasting 6 hours. SR 57227A (1 and 3 mg/kg i.p.) reduces the elevation of the escape failures in the learned helplessness model in rats by 50-60% on the last two days of the avoidance task, and reduces isolation-induced aggressivity in mice by 50 to 85%, an effect which is antagonised by Zacopride (1 mg/kg i.p.)[2].

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

Molecular Weight

248.15

Formula

C10H15Cl2N3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=NC(N2CCC(N)CC2)=CC=C1.[H]Cl

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: 

H2O : 33.33 mg/mL (134.31 mM; Need ultrasonic)

DMSO : 8.33 mg/mL (33.57 mM; Need ultrasonic; 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 4.0298 mL 20.1491 mL 40.2982 mL
5 mM 0.8060 mL 4.0298 mL 8.0596 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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:

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 10 mg/mL (40.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.86%

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 / H2O 1 mM 4.0298 mL 20.1491 mL 40.2982 mL 100.7455 mL
5 mM 0.8060 mL 4.0298 mL 8.0596 mL 20.1491 mL
10 mM 0.4030 mL 2.0149 mL 4.0298 mL 10.0746 mL
15 mM 0.2687 mL 1.3433 mL 2.6865 mL 6.7164 mL
20 mM 0.2015 mL 1.0075 mL 2.0149 mL 5.0373 mL
25 mM 0.1612 mL 0.8060 mL 1.6119 mL 4.0298 mL
30 mM 0.1343 mL 0.6716 mL 1.3433 mL 3.3582 mL
H2O 40 mM 0.1007 mL 0.5037 mL 1.0075 mL 2.5186 mL
50 mM 0.0806 mL 0.4030 mL 0.8060 mL 2.0149 mL
60 mM 0.0672 mL 0.3358 mL 0.6716 mL 1.6791 mL
80 mM 0.0504 mL 0.2519 mL 0.5037 mL 1.2593 mL
100 mM 0.0403 mL 0.2015 mL 0.4030 mL 1.0075 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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SR 57227A 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.

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SR 57227A
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HY-102064
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