515141-51-2

515141-51-2 structure

Name: GW 803430
Chemical Name: 6-(4-chlorophenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]thieno[3,2-d]pyrimidin-4-one
CAS Number: 515141-51-2
Molecular Formula: C₂₅H₂₄ClN₃O₃S
Molecular Weight: 481.99400
Catalog: Signaling Pathways GPCR/G Protein MCHR1 (GPR24)
Create Date: 2016-04-04 23:09:44
Modify Date: 2024-04-03 13:18:54
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].

Name	6-(4-chlorophenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]thieno[3,2-d]pyrimidin-4-one
Synonyms	GW-3430 UNII-4R0136W1PR Guggulsterone QCR-157

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.

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H319
Precautionary Statements	P305 + P351 + P338
RIDADR	NONH for all modes of transport