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SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $159 | 35 days | 35 days | |
| 5 mg | $478 | 35 days | 35 days |
| Description | SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor. |
| Targets&IC50 | 5-HT6 receptor (human):6.5 (pKi), 5-HT1B receptor (human):5.5 (pKi), 5-HT1E receptor (human):<5.4 (pKi), 5-HT1A receptor (human):<5.3 (pKi), 5-HT2A receptor (human):7.01 (pKi), 5-HT7 receptor (human):5.64 (pKi), 5-HT2B receptor (human):7.2 (pKi), 5-HT1D receptor (human):6.32 (pKi), 5-HT2C receptor:9.37 (pKi), 5-HT1F receptor (human):5.35 (pKi) |
| In vitro | SB 243213 dihydrochloride exhibits low affinity (pKi < 6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, and 5-HT7 receptors, weak affinity (pKi < 6.5) for cloned human 5-HT1D and D3 receptors, and moderate affinity (pKi = 6.7) for the cloned human D2 receptor. |
| In vivo | SB 243213 dihydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction. 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. |
| Molecular Weight | 501.33 |
| Formula | C22H21Cl2F3N4O2 |
| Cas No. | 1780372-25-9 |
| Smiles | O=C(N1C2=C(CC1)C=C(C)C(C(F)(F)F)=C2)NC3=CN=C(C=C3)OC4=CC=CN=C4C.Cl.Cl |
| Relative Density. | 1.31g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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