1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB-200646A

SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

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

SB-200646A Chemical Structure

SB-200646A Chemical Structure

CAS No. : 143797-62-0

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 In-stock
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10 mM * 1 mL in DMSO USD 77 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].

IC50 & Target[1][2]

5-HT2B Receptor

7.5 (pKi)

5-HT2C Receptor

6.9 (pKi)

5-HT2A Receptor

5.2 (pKi)

In Vitro

SB200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency[1].

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

In Vivo

SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons[1].
The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1].

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

Animal Model: Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection; daily; for 21 days
Result: Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.
Molecular Weight

302.76

Formula

C15H15ClN4O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC=CN=C1)NC2=CC3=C(N(C)C=C3)C=C2.[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: 

DMSO : 250 mg/mL (825.74 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 3.3029 mL 16.5147 mL 33.0295 mL
5 mM 0.6606 mL 3.3029 mL 6.6059 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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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, 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 1 mM 3.3029 mL 16.5147 mL 33.0295 mL 82.5737 mL
5 mM 0.6606 mL 3.3029 mL 6.6059 mL 16.5147 mL
10 mM 0.3303 mL 1.6515 mL 3.3029 mL 8.2574 mL
15 mM 0.2202 mL 1.1010 mL 2.2020 mL 5.5049 mL
20 mM 0.1651 mL 0.8257 mL 1.6515 mL 4.1287 mL
25 mM 0.1321 mL 0.6606 mL 1.3212 mL 3.3029 mL
30 mM 0.1101 mL 0.5505 mL 1.1010 mL 2.7525 mL
40 mM 0.0826 mL 0.4129 mL 0.8257 mL 2.0643 mL
50 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6515 mL
60 mM 0.0550 mL 0.2752 mL 0.5505 mL 1.3762 mL
80 mM 0.0413 mL 0.2064 mL 0.4129 mL 1.0322 mL
100 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 mL
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  • 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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Product Name:
SB-200646A
Cat. No.:
HY-103129
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