Skip to Content
Merck
All Photos(1)

Key Documents

View All Documentation

Safety Information

S8061

Sigma-Aldrich

SB 242084 dihydrochloride hydrate

≥98% (HPLC), powder

Synonym(s):

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride hydrate, 6-Chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy)pyrid-5-yl]carbamoyl]indoline dihydrochloride hydrate

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C21H19ClN4O2 · 2HCl · xH2O
CAS Number:
181632-25-7
Molecular Weight:
467.78 (anhydrous basis)
MDL number:
MFCD12755727
UNSPSC Code:
12352200
PubChem Substance ID:
24899774
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 15 mg/mL, clear
H2O: 5 mg/mL, clear

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

O.Cl.Cl.Cc1cc2CCN(C(=O)Nc3ccc(Oc4cccnc4C)nc3)c2cc1Cl

InChI

1S/C21H19ClN4O2.2ClH.H2O/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H;1H2

InChI key

SUOZHMLTMKJQNG-UHFFFAOYSA-N

Application

SB 242084 dihydrochloride hydrate was used to study the role of 5-HT2C on food intake behavior of rats.4,5

Biochem/physiol Actions

SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Caution

Hygroscopic

Legal Information

Manufactured and sold with the permission of GlaxoSmithKline Pharmaceuticals

Storage Class Code

13 - Non Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

S8061-5MG:
S8061-25MG:
S8061-VAR:
S8061-BULK:

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number
013M4607V
076M4611V
067K46014
067K46013
067K46012

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Claudia von Meyenburg et al.
Pharmacology, biochemistry, and behavior, 74(2), 505-512 (2002-12-14)
Rats consistently reduce their food intake following injections of bacterial lipopolysaccharides (LPS). Because inhibition of serotonergic (5-HT) activity by 8-OH-DPAT (5-HT(1A) activation) attenuates LPS-induced anorexia, we conducted a series of studies to examine whether other 5-HT-receptors are involved in the
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
S M Bromidge et al.
Journal of medicinal chemistry, 40(22), 3494-3496 (1997-11-14)
V Di Matteo et al.
Neuropharmacology, 38(8), 1195-1205 (1999-08-26)
Electrophysiological techniques and in vivo microdialysis were used to investigate the effect of SB 242084, a potent and selective 5-HT2C receptor antagonist in the control of nigro-striatal and mesolimbic dopaminergic function. Thus, extracellular single unit recordings were performed from neurochemically-identified
G A Kennett et al.
Neuropharmacology, 36(4-5), 609-620 (1997-04-01)
SB 242084 has a high affinity (pKi 9.0) for the cloned human 5-HT2C receptor and 100- and 158-fold selectivity over the closely related cloned human 5-HT2B and 5-HT2A subtypes respectively. SB 242084 had over 100-fold selectivity over a range of
Brigitte S Kopf et al.
Brain research, 1306, 77-84 (2009-09-29)
LPS, a potent activator of the innate immune system, is commonly used to investigate the acute phase response to infection, including anorexia. Serotonin 2C-receptor signaling has been shown to be involved in the mediation of LPS anorexia. Here we used

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service