[CAS NO. 515141-51-2] GW-803430
PRODUCTS SPECIFICATIONS [515141-51-2]
DESCRIPTION [515141-51-2]
Overview
| MDL | MFCD09970889 |
|---|---|
| Molecular Weight | 481.99 |
| Molecular Formula | C25H24ClN3O3S |
| SMILES | O=C1C2=C(C=C(C3=CC=C(Cl)C=C3)S2)N=CN1C4=CC=C(OCCN5CCCC5)C(OC)=C4 |
Summary
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 ( MCH R1 ) antagonist with a pIC 50 of 9.3. GW-803430 is orally active in an animal model of obesity [1] .
IC50 & Target
pIC50: 9.3 (MCH R1) [1]
In Vitro
GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC 50 value of ~13 nM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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%, t
1/2
=11 h) and brain penetration (6:1 brain:plasma concentration) in mice
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
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 Petal Extracts on Lipase, Adipogenesis, Adipolysis, and Central Receptors of Obesity. Evid Based Complement Alternat Med. 2013;2013:145925.
Synonyms