Synonym
GW-803430; GW 803430; GW803430; GW-803430A; GW803430A; GW 803430A; GW3430; GW 3430; GW-3430
IUPAC/Chemical Name
6-(4-Chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one
InChi Key
MWULMTACIBZPGN-UHFFFAOYSA-N
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
SMILES Code
O=C1C2=C(C=C(C3=CC=C(Cl)C=C3)S2)N=CN1C4=CC=C(OCCN5CCCC5)C(OC)=C4
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3.
In vivo activity:
Pretreatment with 3 mg/kg dose of GW803430, significantly reversed the MCH, OT, and MCH+OT mediated reduction in marble burying (Fig. 6A) in mice.
Reference: Neuropharmacology. 2018 Jan;128:22-32. https://pubmed.ncbi.nlm.nih.gov/28888943/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
2.0 |
4.15 |
|
| DMSO |
2.0 |
4.15 |
|
| Ethanol |
2.0 |
4.15 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
482.00
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 |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Sanathara NM, Garau C, Alachkar A, Wang L, Wang Z, Nishimori K, Xu X, Civelli O. Melanin concentrating hormone modulates oxytocin-mediated marble burying. Neuropharmacology. 2018 Jan;128:22-32. doi: 10.1016/j.neuropharm.2017.09.008. Epub 2017 Sep 6. PMID: 28888943; PMCID: PMC5830107.
2. Alachkar A, Alhassen L, Wang Z, Wang L, Onouye K, Sanathara N, Civelli O. Inactivation of the melanin concentrating hormone system impairs maternal behavior. Eur Neuropsychopharmacol. 2016 Nov;26(11):1826-1835. doi: 10.1016/j.euroneuro.2016.08.014. Epub 2016 Sep 9. PMID: 27617778; PMCID: PMC5929110.
In vivo protocol:
1. Sanathara NM, Garau C, Alachkar A, Wang L, Wang Z, Nishimori K, Xu X, Civelli O. Melanin concentrating hormone modulates oxytocin-mediated marble burying. Neuropharmacology. 2018 Jan;128:22-32. doi: 10.1016/j.neuropharm.2017.09.008. Epub 2017 Sep 6. PMID: 28888943; PMCID: PMC5830107.
2. Alachkar A, Alhassen L, Wang Z, Wang L, Onouye K, Sanathara N, Civelli O. Inactivation of the melanin concentrating hormone system impairs maternal behavior. Eur Neuropsychopharmacol. 2016 Nov;26(11):1826-1835. doi: 10.1016/j.euroneuro.2016.08.014. Epub 2016 Sep 9. PMID: 27617778; PMCID: PMC5929110.
1: Rabal O, Amr FI, Oyarzabal J. Novel Scaffold FingerPrint (SFP): applications
in scaffold hopping and scaffold-based selection of diverse compounds. J Chem Inf
Model. 2015 Jan 26;55(1):1-18. doi: 10.1021/ci500542e. Epub 2015 Jan 13. PubMed
PMID: 25558803.
2: Zhang LN, Sinclair R, Selman C, Mitchell S, Morgan D, Clapham JC, Speakman JR.
Effects of a specific MCHR1 antagonist (GW803430) on energy budget and glucose
metabolism in diet-induced obese mice. Obesity (Silver Spring). 2014
Mar;22(3):681-90. doi: 10.1002/oby.20418. Epub 2013 Dec 2. PubMed PMID: 23512845.
3: Karlsson C, Zook M, Ciccocioppo R, Gehlert DR, Thorsell A, Heilig M,
Cippitelli A. Melanin-concentrating hormone receptor 1 (MCH1-R) antagonism:
reduced appetite for calories and suppression of addictive-like behaviors.
Pharmacol Biochem Behav. 2012 Sep;102(3):400-6. doi: 10.1016/j.pbb.2012.06.010.
Epub 2012 Jun 15. PubMed PMID: 22705492.
4: Cippitelli A, Karlsson C, Shaw JL, Thorsell A, Gehlert DR, Heilig M.
Suppression of alcohol self-administration and reinstatement of alcohol seeking
by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats.
Psychopharmacology (Berl). 2010 Sep;211(4):367-75. doi:
10.1007/s00213-010-1891-y. Epub 2010 Jul 14. PubMed PMID: 20628734.
5: Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang
HY, Chen Y, Witkin JM. Preclinical evaluation of melanin-concentrating hormone
receptor 1 antagonism for the treatment of obesity and depression. J Pharmacol
Exp Ther. 2009 May;329(2):429-38. doi: 10.1124/jpet.108.143362. Epub 2009 Jan 30.
PubMed PMID: 19182070.
