Synonym
GSK163090; GSK-163090; GSK 163090
IUPAC/Chemical Name
1-(3-(2-(4-(2-methylquinolin-5-yl)piperazin-1-yl)ethyl)phenyl)imidazolidin-2-one
InChi Key
ANGUXJDGJCHGOG-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H29N5O/c1-19-8-9-22-23(27-19)6-3-7-24(22)29-16-14-28(15-17-29)12-10-20-4-2-5-21(18-20)30-13-11-26-25(30)31/h2-9,18H,10-17H2,1H3,(H,26,31)
SMILES Code
O=C1NCCN1C2=CC=CC(CCN3CCN(C4=C5C=CC(C)=NC5=CC=C4)CC3)=C2
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, not in water
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:
GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
415.54
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:
TBD
1: Leslie CP, Biagetti M, Bison S, Bromidge SM, Di Fabio R, Donati D, Falchi A,
Garnier MJ, Jaxa-Chamiec A, Manchee G, Merlo G, Pizzi DA, Stasi LP, Tibasco J,
Vong A, Ward SE, Zonzini L. Discovery of
1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone
(GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor
antagonist. J Med Chem. 2010 Dec 9;53(23):8228-40. doi: 10.1021/jm100714c. Epub
2010 Nov 5. PubMed PMID: 21053897.
