An antagonist of MCH1
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GW 803430

Item No. 13948

Technical Information
Formal Name
6-(4-chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one
CAS Number
515141-51-2
Synonyms
  • GW 3430
Molecular Formula
C25H24ClN3O3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 2 mg/mlDMSO: 2 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): Slightly soluble
λmax
228, 264, 312 nm
SMILES
O=C1C2=C(C=C(C3=CC=C(Cl)C=C3)S2)N=CN1C4=CC(OC)=C(OCCN5CCCC5)C=C4
InChi Code
InChI=1S/C25H24ClN3O3S/c1-31-22-14-19(8-9-21(22)32-13-12-28-10-2-3-11-28)29-16-27-20-15-23(33-24(20)25(29)30)17-4-6-18(26)7-5-17/h4-9,14-16H,2-3,10-13H2,1H3
InChi Key
MWULMTACIBZPGN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).1 It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.2 GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hertzlog, D.L., Al-Barabzanji, K.A., Bigham, E.C., et alThe discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg. Med. Chem. Lett. 16(18), 4723-4727 (2006).

    2. Gehlert, D.R., Rasmussen, K., Shaw, J., et alPreclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. J. Pharmacol. Exp. Ther. 329(2), 429-438 (2009).