2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB228357

SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.

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

SB228357 Chemical Structure

SB228357 Chemical Structure

CAS No. : 181629-93-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 650 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

SB228357 Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects[1][2].

IC50 & Target[1]

5-HT2A Receptor

6.9 (pKi)

5-HT2C Receptor

9 (pKi)

5-HT2B Receptor

8 (pKi)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
0.01 μM
Compound: 2
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
[PMID: 24900481]
In Vivo

SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2].

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

Animal Model: Male Sprague Dawley rats (200-250 g) injected with Haloperidol[2]
Dosage: 0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg
Administration: Oral administration; for 90 minutes
Result: Significantly reversed Haloperidol-induced catalepsy.
Molecular Weight

431.38

Formula

C22H17F4N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(OC)=C2)NC3=CC(C4=CC=CN=C4)=CC(F)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (289.77 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 2.3181 mL 11.5907 mL 23.1814 mL
5 mM 0.4636 mL 2.3181 mL 4.6363 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: 99.43%

SDS (251 KB)

COA (253 KB) HNMR (273 KB) LCMS (93 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. 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 2.3181 mL 11.5907 mL 23.1814 mL 57.9535 mL
5 mM 0.4636 mL 2.3181 mL 4.6363 mL 11.5907 mL
10 mM 0.2318 mL 1.1591 mL 2.3181 mL 5.7954 mL
15 mM 0.1545 mL 0.7727 mL 1.5454 mL 3.8636 mL
20 mM 0.1159 mL 0.5795 mL 1.1591 mL 2.8977 mL
25 mM 0.0927 mL 0.4636 mL 0.9273 mL 2.3181 mL
30 mM 0.0773 mL 0.3864 mL 0.7727 mL 1.9318 mL
40 mM 0.0580 mL 0.2898 mL 0.5795 mL 1.4488 mL
50 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1591 mL
60 mM 0.0386 mL 0.1932 mL 0.3864 mL 0.9659 mL
80 mM 0.0290 mL 0.1449 mL 0.2898 mL 0.7244 mL
100 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5795 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SB228357 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:

SB228357181629-93-6SB 228357SB-2283575-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SB228357
Cat. No.:
HY-103154
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.