| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
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)
SB 243213 targets the serotonin 5-HT2C receptor, where it acts as an inverse agonist/antagonist. It is highly selective for the 5-HT2C receptor with a pKi of 9.37. By blocking 5-HT2C receptors, it modulates serotonergic signaling pathways involved in mood, appetite, and neuroendocrine function. Its selectivity makes it a valuable tool for studying the specific role of 5-HT2C receptors. |
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| ln Vitro |
Regarding cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, and 5-HT7 receptors, SB 243213 has little affinity (pKi<6.5). The cloned human 5-HT1D and D3 receptors have modest affinity (pKi<6.5), while the cloned human D2 receptor has moderate affinity (pKi=6.7)[1].
In vitro, SB 243213 acts as a selective and high-affinity 5-HT2C receptor antagonist. Its activity is typically assessed by measuring its ability to inhibit agonist-induced calcium mobilization or inositol phosphate accumulation in cells expressing 5-HT2C receptors. The compound shows a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor. Standard in vitro assays include receptor binding studies using radiolabeled ligands such as [3H]-mesulergine and functional assays measuring calcium signaling. |
| ln Vivo |
Rats spend a notable and dose-dependent increase in social contact time (0.1-10 mg/kg, po 1 h pre-test) for 15 minutes in a brightly illuminated, unfamiliar test box when using SB 243213 (0.1-10 mg/kg)[1]. Social contact time is greatly increased by SB 243213 (0.3 mg/kg; po; 1 h pre-test)[1].
In vivo, SB 243213 is orally active and has anxiolytic and antidepressant activity. It has been shown to have an improved anxiolytic profile with a lack of tolerance and withdrawal anxiety. It is used in research on schizophrenia and movement disorders. As a selective 5-HT2C receptor antagonist, it modulates serotonin-regulated pathways in mood, appetite, and neuroendocrine function. |
| Enzyme Assay |
For non-cell-based receptor binding assays, SB 243213 can be evaluated using membrane preparations from cells expressing human 5-HT2C receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-mesulergine. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration. Non-specific binding is determined in the presence of excess unlabeled mesulergine. pKi values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT2C receptors are cultured in appropriate media. For functional assays, intracellular calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and pre-incubated with various concentrations of SB 243213. Receptor activation is stimulated by the addition of a 5-HT2C receptor agonist such as 5-HT. Fluorescence intensity is measured. The reduction in calcium signal compared to control indicates antagonist activity. IC50 or pKb values are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) experimentally naive rats (220-300 g)[1]
Doses: 0.1, 0.3 , 1, 3, 10 mg/kg Route of Administration: PO; 1 hour pre-test Experimental Results: Dose-dependently and Dramatically increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box. For in vivo animal studies, SB 243213 can be administered to rodents via oral gavage. In models of anxiety (e.g., elevated plus maze), behavioral responses are assessed. In models of depression, the forced swim test may be used. In models of schizophrenia, prepulse inhibition and other behavioral tests are performed. Dosing regimens vary depending on the specific model. Blood and tissue samples may be collected for pharmacokinetic analysis. |
| ADME/Pharmacokinetics |
SB 243213 has a molecular formula and weight as described in the literature. It is an orally active compound. The compound should be stored at -20°C for long-term stability. It is soluble in DMSO and can be formulated for both in vitro and in vivo administration. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of SB 243213 has not been extensively reported. As a 5-HT2C receptor antagonist, potential adverse effects may include modulation of serotonergic signaling. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies.
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| References | |
| Additional Infomation |
SB 243213 is an indole carboxylic acid.
SB 243213 (CAS 200940-22-3) is an orally active, selective, and high-affinity 5-HT2C receptor antagonist. It has a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor. It has anxiolytic and antidepressant activity. It is used in research on schizophrenia and movement disorders. It is available for research purposes only. |
| Molecular Formula |
C22H19F3N4O2
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|---|---|
| Molecular Weight |
428.41
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| Exact Mass |
428.146
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| CAS # |
200940-22-3
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| Related CAS # |
SB 243213 hydrochloride;200940-23-4;SB 243213 dihydrochloride;1780372-25-9
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| PubChem CID |
443391
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| Appearance |
White to off-white solid powder
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| LogP |
5.577
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1C(F)(F)F)N(CC2)C(=O)NC3=CN=C(C=C3)OC4=C(N=CC=C4)C
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| InChi Key |
ZETBBVYSBABLHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19F3N4O2/c1-13-10-15-7-9-29(18(15)11-17(13)22(23,24)25)21(30)28-16-5-6-20(27-12-16)31-19-4-3-8-26-14(19)2/h3-6,8,10-12H,7,9H2,1-2H3,(H,28,30)
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| Chemical Name |
5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (291.78 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2334 mL | 1.1671 mL | 2.3342 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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