SB-243213
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MedKoo CAT#: 574397

CAS#: 200940-22-3

Description: SB-243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist. SB-243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

Chemical Structure

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SB-243213
CAS# 200940-22-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574397
Name: SB-243213
CAS#: 200940-22-3
Chemical Formula: C22H19F3N4O2
Exact Mass: 428.15
Molecular Weight: 428.420
Elemental Analysis: C, 61.68; H, 4.47; F, 13.30; N, 13.08; O, 7.47

Price and Availability

Size Price Availability Quantity
5mg USD 400 2 Weeks
10mg USD 600 2 Weeks
25mg USD 1000 2 Weeks
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Synonym: SB-243213, SB243213, SB 243213

IUPAC/Chemical Name: 5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide

InChi Key: ZETBBVYSBABLHL-UHFFFAOYSA-N

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)

SMILES Code: O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: SB-243213 is a 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.
In vitro activity: To be determined
In vivo activity: In adult rats, SB-243213 significantly reduced the time spent in rapid-eye-movement (REM) sleep following subcutaneous administration. SB-243213 did not reverse the changes in sleep and waking induced by the serotonin agonist DOI. 5-HT(2A) receptor mechanisms are likely accountable for DOI-induced alterations in waking and slow wave sleep. Reference: Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. https://pubmed.ncbi.nlm.nih.gov/17059817/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 297.78

Preparing Stock Solutions

The following data is based on the product molecular weight 428.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. De Deurwaerdère P, Le Moine C, Chesselet MF. Selective blockade of serotonin 2C receptor enhances Fos expression specifically in the striatum and the subthalamic nucleus within the basal ganglia. Neurosci Lett. 2010 Jan 22;469(2):251-5. doi: 10.1016/j.neulet.2009.12.006. Epub 2009 Dec 11. PMID: 20004702. 2. Monti JM, Jantos H. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. doi: 10.1016/j.ejphar.2006.09.027. Epub 2006 Sep 23. PMID: 17059817.
In vitro protocol: 1. De Deurwaerdère P, Le Moine C, Chesselet MF. Selective blockade of serotonin 2C receptor enhances Fos expression specifically in the striatum and the subthalamic nucleus within the basal ganglia. Neurosci Lett. 2010 Jan 22;469(2):251-5. doi: 10.1016/j.neulet.2009.12.006. Epub 2009 Dec 11. PMID: 20004702. 2. Monti JM, Jantos H. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. doi: 10.1016/j.ejphar.2006.09.027. Epub 2006 Sep 23. PMID: 17059817.
In vivo protocol:

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1. Bromidge et al (2000) Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic a J.Med.Chem. 43 1123 PMID: 10737744

2. Wood et al (2001) SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology 41 186 PMID: 11489455

3. Berg et al (2006) Differential effects of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxyl]-5-pyridyl]carbamoyl]-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine2C receptor-mediated responses. J.Pharmacol.Exp.Ther. 319 260 PMID: 16807362