GSK-239512 | CAS#720691-69-0 | H3 Receptor Antagonist

MedKoo Cat#: 525213 | Name: GSK-239512

Description:

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

GSK-239512 is a novel histamine H(3) receptor antagonist. GSK-239512 was developed for the treatment of cognitive dysfunction in neurodegenerative disorders with mild to moderate Alzheimer's disease.

Chemical Structure

GSK-239512

CAS#720691-69-0

Theoretical Analysis

MedKoo Cat#: 525213

Name: GSK-239512

CAS#: 720691-69-0

Chemical Formula: C23H27N3O2

Exact Mass: 377.2103

Molecular Weight: 377.48

Elemental Analysis: C, 73.18; H, 7.21; N, 11.13; O, 8.48

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.

Bulk Inquiry

Related CAS #

No Data

Synonym

GSK-239512; GSK239512; GSK 239512;

IUPAC/Chemical Name

2-Pyrrolidinone, 1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-3-pyridinyl)-

InChi Key

YFRBKEVUUCQYOW-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H27N3O2/c27-23-5-2-12-26(23)20-7-9-22(24-16-20)28-21-8-6-17-10-13-25(19-3-1-4-19)14-11-18(17)15-21/h6-9,15-16,19H,1-5,10-14H2

SMILES Code

O=C1CCCN1c2ccc(Oc3ccc4CCN(CCc4c3)C5CCC5)nc2

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 377.48 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

1: Kubo M, Kishi T, Matsunaga S, Iwata N. Histamine H3 Receptor Antagonists for Alzheimer's Disease: A Systematic Review and Meta-Analysis of Randomized Placebo-Controlled Trials. J Alzheimers Dis. 2015;48(3):667-71. doi: 10.3233/JAD-150393. PubMed PMID: 26402104. 2: Jarskog LF, Lowy MT, Grove RA, Keefe RS, Horrigan JP, Ball MP, Breier A, Buchanan RW, Carter CS, Csernansky JG, Goff DC, Green MF, Kantrowitz JT, Keshavan MS, Laurelle M, Lieberman JA, Marder SR, Maruff P, McMahon RP, Seidman LJ, Peykamian MA. A Phase II study of a histamine H₃ receptor antagonist GSK239512 for cognitive impairment in stable schizophrenia subjects on antipsychotic therapy. Schizophr Res. 2015 May;164(1-3):136-42. doi: 10.1016/j.schres.2015.01.041. Epub 2015 Feb 24. PubMed PMID: 25728831. 3: Xu J, Hilpert J, Wu K, van Hecke B, Collins G, Patel A, Mohindra R, Davies MJ, Xu Y, Thompson P. An adaptive design to investigate the effect of ketoconazole on pharmacokinetics of GSK239512 in healthy male volunteers. J Clin Pharmacol. 2015 May;55(5):505-11. doi: 10.1002/jcph.441. Epub 2015 Feb 4. PubMed PMID: 25470032. 4: Ashworth S, Berges A, Rabiner EA, Wilson AA, Comley RA, Lai RY, Boardley R, Searle G, Gunn RN, Laruelle M, Cunningham VJ. Unexpectedly high affinity of a novel histamine H(3) receptor antagonist, GSK239512, in vivo in human brain, determined using PET. Br J Pharmacol. 2014 Mar;171(5):1241-9. doi: 10.1111/bph.12505. PubMed PMID: 24670146; PubMed Central PMCID: PMC3952801. 5: Grove RA, Harrington CM, Mahler A, Beresford I, Maruff P, Lowy MT, Nicholls AP, Boardley RL, Berges AC, Nathan PJ, Horrigan JP. A randomized, double-blind, placebo-controlled, 16-week study of the H3 receptor antagonist, GSK239512 as a monotherapy in subjects with mild-to-moderate Alzheimer's disease. Curr Alzheimer Res. 2014 Jan;11(1):47-58. PubMed PMID: 24359500. 6: Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD. Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5. PubMed PMID: 24269482. 7: Nathan PJ, Boardley R, Scott N, Berges A, Maruff P, Sivananthan T, Upton N, Lowy MT, Nestor PJ, Lai R. The safety, tolerability, pharmacokinetics and cognitive effects of GSK239512, a selective histamine H₃ receptor antagonist in patients with mild to moderate Alzheimer's disease: a preliminary investigation. Curr Alzheimer Res. 2013 Mar;10(3):240-51. PubMed PMID: 23521503.