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Submit ReviewGW 803430
Description: MCH1 antagonist
Chemical Name: 6-(4-Chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one
Purity: ≥95% (HPLC)
Biological Activity for GW 803430
GW 803430 is a selective melanin-concentrating hormone receptor 1 (MCH1) antagonist (IC50 = 9.3 nM). Displays antiobesity and antidepressant-like effects in rats and mice. Orally active.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data for GW 803430
| M. Wt | 481.99 |
| Formula | C25H24ClN3O3S |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 515141-51-2 |
| PubChem ID | 9826520 |
| InChI Key | MWULMTACIBZPGN-UHFFFAOYSA-N |
| Smiles | ClC(C=C3)=CC=C3C(S2)=CC1=C2C(N(C4=CC(OC)=C(OCCN5CCCC5)C=C4)C=N1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GW 803430
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 14.75 | 25 |
Preparing Stock Solutions for GW 803430
The following data is based on the product molecular weight 481.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 8.3 mL | 41.49 mL | 82.99 mL |
| 1.25 mM | 1.66 mL | 8.3 mL | 16.6 mL |
| 2.5 mM | 0.83 mL | 4.15 mL | 8.3 mL |
| 12.5 mM | 0.17 mL | 0.83 mL | 1.66 mL |
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Product Datasheets for GW 803430
References for GW 803430
References are publications that support the biological activity of the product.
Rivera et al (2008) Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity. Curr.Med.Chem. 15 1025 PMID: 18393860
Gehlert et al (2009) Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. J.Pharmacol.Exp.Ther. 329 429 PMID: 19182070
If you know of a relevant reference for GW 803430, please let us know.
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Keywords: GW 803430, GW 803430 supplier, glaxosmithkline, melanin, concentrating, hormone, receptors, mchr1, antagonists, antiobesity, obese, GW803430, Melanin-concentrating, Hormone, Receptors, 4242, Tocris Bioscience
Citations for GW 803430
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.