GW 803430
Modify Date: 2024-04-03 13:18:54
GW 803430 structure
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Common Name | GW 803430 | ||
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| CAS Number | 515141-51-2 | Molecular Weight | 481.99400 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H24ClN3O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of GW 803430GW-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 |
|---|---|
| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C25H24ClN3O3S |
|---|---|
| Molecular Weight | 481.99400 |
| Exact Mass | 481.12300 |
| PSA | 84.83000 |
| LogP | 5.18870 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302-H319 |
| Precautionary Statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |
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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... |
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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... |
| GW-3430 |
| UNII-4R0136W1PR |
| Guggulsterone |
| QCR-157 |