GW 803430

Names

[ Name ]:
GW 803430

[Synonym ]:
GW-3430
UNII-4R0136W1PR
Guggulsterone
QCR-157

Biological Activity

[Description]:

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> MCHR1 (GPR24)

Research Areas >> Metabolic Disease

[Target]

pIC50: 9.3 (MCH R1)[1]

[In Vitro]

GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50 value of ~13 nM[2].

[In Vivo]

GW-803430 (0.3, 3, and 15 mg/kg ; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls[1]. GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t1/2=11 h) and brain penetration (6:1 brain:plasma concentration) in mice[1]. Animal Model: High fat diet-induced obese AKR/J mice[1] Dosage: 0.3, 3, and 15 mg/kg Administration: Orally, qd,12 days Result: Caused a sustained dose-dependent weight loss of -6.2%, -12.1%, and -13.1%, respectively, relative to vehicle controls.

[References]

[1]. Hertzog DL, et al. The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7.

[2]. Velusami CC, et al. Effect of Nelumbo nucifera Petal Extracts on Lipase, Adipogenesis, Adipolysis, and Central Receptors of Obesity. Evid Based Complement Alternat Med. 2013;2013:145925.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₄ClN₃O₃S

[ Molecular Weight ]:
481.99400

[ Exact Mass ]:
481.12300

[ PSA ]:
84.83000

[ LogP ]:
5.18870

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H319

[ Precautionary Statements ]:
P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport

Articles

Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression.

J. Pharmacol. Exp. Ther. 329(2) , 429-38, (2009)

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 i...

Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats.

Psychopharmacology 211(4) , 367-75, (2010)

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 effe...