2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB 243213

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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.

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SB 243213 Chemical Structure

SB 243213 Chemical Structure

CAS No. : 200940-22-3

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Based on 1 publication(s) in Google Scholar

Other Forms of SB 243213:

SB 243213 Related Antibodies

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View All 5-HT Receptor Isoform Specific Products:

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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

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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[1].

IC50 & Target[1]

Human 5-HT2C Receptor

9.37 (pKi)

human 5-HT1A Receptor

<5.3 (pKi)

human 5-HT1B Receptor

5.5 (pKi)

human 5-HT1D Receptor

6.32 (pKi)

human 5-HT1E Receptor

<5.4 (pKi)

human 5-HT1F Receptor

5.35 (pKi)

Human 5-HT2A Receptor

7.01 (pKi)

human 5-HT2B Receptor

7.2 (pKi)

Human 5-HT6 Receptor

6.5 (pKi)

Human 5-HT7 Receptor

5.64 (pKi)

In Vitro

SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=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.

SB 243213 Related Antibodies
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.
Molecular Weight

428.41

Formula

C22H19F3N4O2
CAS No.
Appearance

Solid

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 : 125 mg/mL (291.78 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 2.3342 mL 11.6711 mL 23.3421 mL
5 mM 0.4668 mL 2.3342 mL 4.6684 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, 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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, 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 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:

SB 243213200940-22-3SB243213SB-2432135-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorOrally5-hydroxytryptamineanxiolyticprofileschizophreniamotordisordersneurotransmitterreceptorsenzymesionchannelsInhibitorinhibitorinhibit

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