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Key Documents

SML0230

Sigma-Aldrich

GW-803430

≥98% (HPLC)

Synonym(s):

6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one, GW-3430, GW-803430A

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About This Item

Empirical Formula (Hill Notation):
C25H24ClN3O3S
CAS Number:
515141-51-2
Molecular Weight:
481.99
UNSPSC Code:
51111800
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥4 mg/mL at warmed to 60 °C

originator

GlaxoSmithKline

storage temp.

2-8°C

InChI

1S/C25H24ClN3O3S/c1-31-22-14-19(8-9-21(22)32-13-12-28-10-2-3-11-28)29-16-27-20-15-23(33-24(20)25(29)30)17-4-6-18(26)7-5-17/h4-9,14-16H,2-3,10-13H2,1H3

InChI key

MWULMTACIBZPGN-UHFFFAOYSA-N

Application

GW-803430 may be used in MCHR1-mediated cell signaling studies.

Biochem/physiol Actions

GW-803430 antagonizes central MCHR1 and produces anxiolytic, anti-depressant and anti-obesity effects in rats and mice. It also controls the alcohol-seeking behavior in rats and is a promising treatment for alcohol use-related disorders.
GW-803430 is a centraly active and selective melanin-concentrating hormone receptor (MCHR) 1 antagonist

Features and Benefits

This compound is featured on the Melanin-Concentrating Hormone Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302,H319

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
012M4604V

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Andrea Cippitelli et al.
Psychopharmacology, 211(4), 367-375 (2010-07-16)
Melanin-concentrating hormone (MCH) is involved in regulation of appetitive behaviors as well as emotional reactivity and reward, behavioral domains relevant to alcohol addiction. We evaluated the effects of the non-peptide MCH1 receptor antagonist, GW803430 [6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one; 3-30 mg/kg, i.p.] on alcohol-related
Donald R Gehlert et al.
The Journal of pharmacology and experimental therapeutics, 329(2), 429-438 (2009-02-03)
The mammalian neuropeptide, melanin-concentrating hormone, interacts with two G protein-coupled receptors, melanin-concentrating hormone receptor (MCHR) 1 and MCHR2; however, only MCHR1 is expressed in rats and mice. In the present study, we evaluated MCHR1 antagonism in preclinical models believed to

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