MedKoo Cat#: 525210 | Name: GSK-215083

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is tested for the treatment of Alzheimer's disease, and coupled with 11C, as a PET ligand for identification of occupancy of the 5HT6 receptor. GSK 215083 is a quinoline based compounds that acts by antagonising the 5-HT6 receptor. Preclinical studies conducted of the ligand indicated that it binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in the frontal cortex.

Chemical Structure

GSK-215083
GSK-215083
CAS#607742-80-3

Theoretical Analysis

MedKoo Cat#: 525210

Name: GSK-215083

CAS#: 607742-80-3

Chemical Formula: C20H20FN3O2S

Exact Mass: 385.1260

Molecular Weight: 385.46

Elemental Analysis: C, 62.32; H, 5.23; F, 4.93; N, 10.90; O, 8.30; S, 8.32

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
GSK-215083; GSK 215083; GSK215083;
IUPAC/Chemical Name
Quinoline, 3-((3-fluorophenyl)sulfonyl)-8-(4-methyl-1-piperazinyl)-
InChi Key
PXVJEDOZGDZJQY-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H20FN3O2S/c1-23-8-10-24(11-9-23)19-7-2-4-15-12-18(14-22-20(15)19)27(25,26)17-6-3-5-16(21)13-17/h2-7,12-14H,8-11H2,1H3
SMILES Code
CN1CCN(C2=C3N=CC(S(=O)(C4=CC=CC(F)=C4)=O)=CC3=CC=C2)CC1
Appearance
Solid powder
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 385.46 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.

Recalculate based on batch purity %
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
1: Parker CA, Rabiner EA, Gunn RN, Searle G, Martarello L, Comley RA, Davy M, Wilson AA, Houle S, Mizrahi R, Laruelle M, Cunningham VJ. Human Kinetic Modeling of the 5HT6 PET Radioligand 11C-GSK215083 and Its Utility for Determining Occupancy at Both 5HT6 and 5HT2A Receptors by SB742457 as a Potential Therapeutic Mechanism of Action in Alzheimer Disease. J Nucl Med. 2015 Dec;56(12):1901-9. doi: 10.2967/jnumed.115.162743. Epub 2015 Sep 17. PubMed PMID: 26383152. 2: Becker G, Colomb J, Sgambato-Faure V, Tremblay L, Billard T, Zimmer L. Preclinical evaluation of [18F]2FNQ1P as the first fluorinated serotonin 5-HT6 radioligand for PET imaging. Eur J Nucl Med Mol Imaging. 2015 Mar;42(3):495-502. doi: 10.1007/s00259-014-2936-y. Epub 2014 Oct 21. PubMed PMID: 25331460. 3: Chopra A. [(11)C]-[N-Methyl]3-[(3-fluorophenyl)sulfonyl]-8-(4-methyl-1-piperazinyl)quinolin e. 2012 Feb 06 [updated 2012 Apr 27]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. Available from http://www.ncbi.nlm.nih.gov/books/NBK92499/ PubMed PMID: 22553893. 4: Parker CA, Gunn RN, Rabiner EA, Slifstein M, Comley R, Salinas C, Johnson CN, Jakobsen S, Houle S, Laruelle M, Cunningham VJ, Martarello L. Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor. J Nucl Med. 2012 Feb;53(2):295-303. doi: 10.2967/jnumed.111.093419. Epub 2012 Jan 5. PubMed PMID: 22223878. 5: Comley RA, Salinas C, Mizrahi R, Vitcu I, Ng A, Hallett W, Keat N, Wilson AA, Rabiner EA, Laruelle M, Houle S. Biodistribution and radiation dosimetry of the serotonin 5-HT₆ ligand [¹¹C]GSK215083 determined from human whole-body PET. Mol Imaging Biol. 2012 Aug;14(4):517-21. doi: 10.1007/s11307-011-0523-1. PubMed PMID: 22076076. 6: Hirano K, Searle KL, Nasir S, Aw CC, Browne ER, Rutter AR. In vivo 5-HT(6) receptor occupancy by antipsychotic drugs in the rat brain. Neurosci Lett. 2011 Oct 10;503(3):240-3. doi: 10.1016/j.neulet.2011.08.044. Epub 2011 Aug 27. PubMed PMID: 21896308.