LY450108

AMPA receptor potentiator CAS# 376594-67-1

LY450108

Catalog No. BCC1725----Order now to get a substantial discount!

Product Name & Size Price Stock
LY450108: 5mg $276 In Stock
LY450108: 10mg Please Inquire In Stock
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Quality Control of LY450108

Number of papers citing our products

Chemical structure

LY450108

3D structure

Chemical Properties of LY450108

Cas No. 376594-67-1 SDF Download SDF
PubChem ID 9843690 Appearance Powder
Formula C19H22F2N2O3S M.Wt 396.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 50 mg/mL (126.12 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 3,5-difluoro-N-[4-[(2R)-1-(propan-2-ylsulfonylamino)propan-2-yl]phenyl]benzamide
SMILES CC(C)S(=O)(=O)NCC(C)C1=CC=C(C=C1)NC(=O)C2=CC(=CC(=C2)F)F
Standard InChIKey ACOXQYLJOQAHST-ZDUSSCGKSA-N
Standard InChI InChI=1S/C19H22F2N2O3S/c1-12(2)27(25,26)22-11-13(3)14-4-6-18(7-5-14)23-19(24)15-8-16(20)10-17(21)9-15/h4-10,12-13,22H,11H2,1-3H3,(H,23,24)/t13-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LY450108

DescriptionLY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator. IC50 value: Target: AMPA receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). Recent evidence has shown that in addition to modulating fast synaptic plasticity and memory processes, AMPA receptor potentiators alter downstream signalling pathways and may thereby have utility in other CNS disorders.

References:
[1]. Simon E Ward1, Benjamin D Bax, Mark Harries. Challenges for and current status of research into positive modulators of AMPA receptors. British Journal of Pharmacology. 2010,160(2):181-190. [2]. O'Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson's disease. Curr Drug Targets. 2007 May;8(5):603-20. [3]. Jhee SS, Chappell AS, Zarotsky V, et al. Multiple-dose plasma pharmacokinetic and safety study of LY450108 and LY451395 (AMPA receptor potentiators) and their concentration in cerebrospinal fluid in healthy human subjects. J Clin Pharmacol. 2006 Apr;46(4):424-32. [4]. Douglas A. Schober, Martin B. Gill, Hong Yu, et al. Transmembrane AMPA Receptor Regulatory Proteins and Cornichon-2 Allosterically Regulate AMPA Receptor Antagonists and Potentiators. The Journal of Biological Chemistry, 286, 13134-13142.

LY450108 Dilution Calculator

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LY450108 Molarity Calculator

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Preparing Stock Solutions of LY450108

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5224 mL 12.6119 mL 25.2239 mL 50.4477 mL 63.0597 mL
5 mM 0.5045 mL 2.5224 mL 5.0448 mL 10.0895 mL 12.6119 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 5.0448 mL 6.306 mL
50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.009 mL 1.2612 mL
100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.5045 mL 0.6306 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on LY450108

LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator. AMPA receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). Recent evidence has shown that in addition to modulating fast synaptic plasticity and memory processes, AMPA receptor potentiators alter downstream signalling pathways and may thereby have utility in other CNS disorders.

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References on LY450108

Multiple-dose plasma pharmacokinetic and safety study of LY450108 and LY451395 (AMPA receptor potentiators) and their concentration in cerebrospinal fluid in healthy human subjects.[Pubmed:16554450]

J Clin Pharmacol. 2006 Apr;46(4):424-32.

The objective of this study was to measure the steady-state cerebrospinal fluid (CSF) concentration of LY450108 and LY451395 (positive modulators of AMPA receptors) in healthy subjects after the administration of 1 mg and 5 mg. Secondary objectives included the evaluation of safety, pharmacokinetics, and steady-state ratio of plasma:CSF concentrations of LY450108 and LY451395 after multiple dosing. This study was an open-label, multiple oral dose study evaluating 1 mg and 5 mg LY450108 and 1 mg and 5 mg LY451395 in 12 (3 subjects per dosing group) healthy subjects, aged 18 to 49 years. Twelve healthy male subjects completed the study. LY450108 and LY451395 were quantifiable in CSF after 1-mg and 5-mg multiple-dose administrations with plasma:CSF ratio of 82:1 and 44:1, respectively. LY450108 and LY451395 1 mg and 5 mg were measured in the CSF. Single and multiple oral doses of LY450108 and LY451395 were determined to be safe and well tolerated in healthy subjects.

Description

LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator.

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