Cat. No.: HY-103112B

SB 243213

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Based on 1 Customer Validation

SB 243213 is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

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

Purity: 99.39%
CAS No.: 200940-22-3
Formula: C₂₂H₁₉F₃N₄O₂
Molecular Weight:428.41

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SB 243213 Chemical Structure

CAS No.: 200940-22-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Human 5-HT_2C Receptor

9.37 (pKi)

5-HT_2C Receptor

human 5-HT_1A Receptor

<5.3 (pKi)

human 5-HT_1B Receptor

5.5 (pKi)

human 5-HT_1D Receptor

6.32 (pKi)

human 5-HT_1E Receptor

<5.4 (pKi)

human 5-HT_1F Receptor

5.35 (pKi)

Human 5-HT_2A Receptor

7.01 (pKi)

human 5-HT_2B Receptor

7.2 (pKi)

Human 5-HT₆ Receptor

6.5 (pKi)

Human 5-HT₇ Receptor

5.64 (pKi)

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.7 nM Compound: 1, SB-243213	Displacement of [3H]mesulergine at human cloned 5HT2C receptor expressed in CHOK1 cell Displacement of [3H]mesulergine at human cloned 5HT2C receptor expressed in CHOK1 cell	[PMID: 18602261]

In Vitro

SB 243213 shows little affinity (pK_i<6) for cloned human 5-HT_1A, 5-HT_1B, 5-HT_1E, 5- HT_1F and 5-HT₇ receptors. It shows weak affinity (pK_i<6.5) for the cloned human 5-HT_1D and D3 receptors and moderate affinity (pK_i=6.7) for the cloned human D2 receptor^[1].

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

In Vivo

SB 243213 (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box^[1].
SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction^[1].

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

Animal Model:

Male Sprague-Dawley experimentally naive rats (220-300 g)^[1]
Dosage:

0.1, 0.3, 1, 3, 10 mg/kg
Administration:

PO; 1 hour pre-test
Result:

Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.

Chemical Information

CAS No. 200940-22-3
Appearance Solid
Molecular Weight 428.41
Formula C₂₂H₁₉F₃N₄O₂
Color White to off-white
SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (233.42 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3342 mL

11.6711 mL

23.3421 mL

5 mM

0.4668 mL

2.3342 mL

4.6684 mL

10 mM

0.2334 mL

1.1671 mL

2.3342 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3342 mL	11.6711 mL	23.3421 mL	58.3553 mL
	5 mM	0.4668 mL	2.3342 mL	4.6684 mL	11.6711 mL
	10 mM	0.2334 mL	1.1671 mL	2.3342 mL	5.8355 mL
	15 mM	0.1556 mL	0.7781 mL	1.5561 mL	3.8904 mL
	20 mM	0.1167 mL	0.5836 mL	1.1671 mL	2.9178 mL
	25 mM	0.0934 mL	0.4668 mL	0.9337 mL	2.3342 mL
	30 mM	0.0778 mL	0.3890 mL	0.7781 mL	1.9452 mL
	40 mM	0.0584 mL	0.2918 mL	0.5836 mL	1.4589 mL
	50 mM	0.0467 mL	0.2334 mL	0.4668 mL	1.1671 mL
	60 mM	0.0389 mL	0.1945 mL	0.3890 mL	0.9726 mL
	80 mM	0.0292 mL	0.1459 mL	0.2918 mL	0.7294 mL
	100 mM	0.0233 mL	0.1167 mL	0.2334 mL	0.5836 mL

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SB 243213

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

5-HT Receptor Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SB 243213

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

5-HT Receptor Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SB 243213 Related Classifications

HY-103112B Related Classifications