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Cat. No.: HY-103112A

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SB 243213 dihydrochloride

SB 243213 dihydrochloride 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 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

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

CAS No.: 1780372-25-9
Formula: C₂₂H₂₁Cl₂F₃N₄O₂
Molecular Weight:501.33

Storage:

4°C, sealed storage, away from moisture

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

SB 243213 dihydrochloride Chemical Structure

CAS No.: 1780372-25-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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 :

In Vitro

SB 243213 dihydrochloride 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].
SB 243213 dihydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels^[1].

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

In Vivo

SB 243213 dihydrochloride (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 dihydrochloride (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:

p.o.; 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. 1780372-25-9
Appearance Solid
Molecular Weight 501.33
Formula C₂₂H₂₁Cl₂F₃N₄O₂
Color Light yellow to yellow
SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl.[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)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]

Calculators

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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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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SB 243213 dihydrochloride

All 5-HT Receptor Isoforms