SB-243213 | CAS# 200940-22-3 | 5-HT2C inverse agonist

MedKoo Cat#: 574397 | Name: SB-243213

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

SB-243213

CAS#200940-22-3

Theoretical Analysis

MedKoo Cat#: 574397

Name: SB-243213

CAS#: 200940-22-3

Chemical Formula: C22H19F3N4O2

Exact Mass: 428.1460

Molecular Weight: 428.42

Elemental Analysis: C, 61.68; H, 4.47; F, 13.30; N, 13.08; O, 7.47

Price and Availability

Size	Price	Availability
5mg	USD 400.00	2 Weeks
10mg	USD 600.00	2 Weeks
25mg	USD 1,000.00	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/

	Solvent	mg/mL	mM
Solubility
	DMSO	125.0	297.78

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

In vivo protocol:

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