GSK1614343 | CAS#1092476-84-0 | Ghrelin Receptor Antagonist

MedKoo Cat#: 531868 | Name: GSK1614343

Description:

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

GSK1614343 is a novel selective and potent GHSR antagonist with no partial agonist properties. GSK1614343 produces an unexpected increase of food intake and body weight in rodents and dogs. GSK1614343 selectively reduced the pro-opiomelanocortin mRNA levels in rat hypothalami chronically treated with the compound. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models.

Chemical Structure

GSK1614343

CAS#1092476-84-0

Theoretical Analysis

MedKoo Cat#: 531868

Name: GSK1614343

CAS#: 1092476-84-0

Chemical Formula: C22H23F6N5O

Exact Mass: 487.1807

Molecular Weight: 487.45

Elemental Analysis: C, 54.21; H, 4.76; F, 23.39; N, 14.37; O, 3.28

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

GSK1614343; GSK 1614343; GSK-1614343.

IUPAC/Chemical Name

(2R)-2-[(8aR)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-N'-[3,5-bis(trifluoromethyl)phenyl]-2-pyridin-3-ylacetohydrazide

InChi Key

QNOSCJDGJKVFJR-RTBURBONSA-N

InChi Code

InChI=1S/C22H23F6N5O/c23-21(24,25)15-9-16(22(26,27)28)11-17(10-15)30-31-20(34)19(14-3-1-5-29-12-14)33-8-7-32-6-2-4-18(32)13-33/h1,3,5,9-12,18-19,30H,2,4,6-8,13H2,(H,31,34)/t18-,19-/m1/s1

SMILES Code

O=C(NNC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)[C@H](N2C[C@](CCC3)([H])N3CC2)C4=CC=CN=C4

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 487.45 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: Kim JN, Nam JH, Lee JR, Kim SC, Kwon YK, Kim BJ. Rikkunshito Depolarizes Pacemaker Potentials of Cultured Interstitial Cells of Cajal through Ghrelin Receptors in Murine Small Intestine. Digestion. 2020;101(3):227-238. doi: 10.1159/000498986. Epub 2019 Mar 19. PMID: 30889598. 2: Costantini VJ, Vicentini E, Sabbatini FM, Valerio E, Lepore S, Tessari M, Sartori M, Michielin F, Melotto S, Bifone A, Pich EM, Corsi M. GSK1614343, a novel ghrelin receptor antagonist, produces an unexpected increase of food intake and body weight in rodents and dogs. Neuroendocrinology. 2011;94(2):158-68. doi: 10.1159/000328968. Epub 2011 Jul 22. Erratum in: Neuroendocrinology. 2012;95(3):247. Bifone, Angelo [added]. PMID: 21778696. 3: Perdonà E, Faggioni F, Buson A, Sabbatini FM, Corti C, Corsi M. Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors. Eur J Pharmacol. 2011 Jan 10;650(1):178-83. doi: 10.1016/j.ejphar.2010.10.042. Epub 2010 Oct 29. PMID: 21034740.