LY451395Allosteric modulator CAS# 375345-95-2 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 375345-95-2 | SDF | Download SDF |
| PubChem ID | 9889366 | Appearance | Powder |
| Formula | C21H30N2O4S2 | M.Wt | 438.6 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Mibampator | ||
| Solubility | DMSO : ≥ 25 mg/mL (57.00 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-[(2R)-2-[4-[4-[2-(methanesulfonamido)ethyl]phenyl]phenyl]propyl]propane-2-sulfonamide | ||
| SMILES | CC(C)S(=O)(=O)NCC(C)C1=CC=C(C=C1)C2=CC=C(C=C2)CCNS(=O)(=O)C | ||
| Standard InChIKey | ULRDYYKSPCRXAJ-KRWDZBQOSA-N | ||
| Standard InChI | InChI=1S/C21H30N2O4S2/c1-16(2)29(26,27)23-15-17(3)19-9-11-21(12-10-19)20-7-5-18(6-8-20)13-14-22-28(4,24)25/h5-12,16-17,22-23H,13-15H2,1-4H3/t17-/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. |
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| 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. |
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| 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. | ||
| Description | LY451395(Mibampator) is a potent and highly selective potentiator of the AMPA receptors.
IC50 value:
Target: AMPA receptor potentiator
in vitro:
in vivo: Incubation of LY451395 with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies of the preclinical species [1]. LY404187 and LY451395 reverses the central effects of an acutely intoxicating dose of ethanol in the rat. LY451395 significantly and dose-dependently reversed ethanol-induced deficits in both motor coordination and disruptions in an operant task where animals were trained to press a lever for food reward [2]. References: | |||||
LY451395 Dilution Calculator
LY451395 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.28 mL | 11.3999 mL | 22.7998 mL | 45.5996 mL | 56.9995 mL |
| 5 mM | 0.456 mL | 2.28 mL | 4.56 mL | 9.1199 mL | 11.3999 mL |
| 10 mM | 0.228 mL | 1.14 mL | 2.28 mL | 4.56 mL | 5.7 mL |
| 50 mM | 0.0456 mL | 0.228 mL | 0.456 mL | 0.912 mL | 1.14 mL |
| 100 mM | 0.0228 mL | 0.114 mL | 0.228 mL | 0.456 mL | 0.57 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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LY451395 (Mibampator) is a powerful, highly selective and biarylsulfonamide potentiator of AMPA receptors [1].
LY451395 (Mibampator) has been found to be a potent, selective and centrally active positive allosteric modulators of AMPA receptor-mediated neurotransmission, which enhances ion channel flux in the presence of agonist by inhibiting desensitization and deactivation of the receptors. In addition, LY451395 has been revealed to enhance synaptic transmission. Besides, LY451395 has been reported to attenuate the response to acute ethanol administration in the rat in vivo [1]. Moreover, the in vivo metabolisms of LY451395 in mouse, rat, dog and human have produced several phase 1 oxidative metabolites [2].
References:
[1] Jones N1, Messenger MJ, O'Neill MJ, Oldershaw A, Gilmour G, Simmons RM, Iyengar S, Libri V, Tricklebank M, Williams SC. AMPA receptor potentiation can prevent ethanol-induced intoxication. Neuropsychopharmacology. 2008 Jun;33(7):1713-23. Epub 2007 Sep 12.
[2] Zmijewski M1, Gillespie TA, Jackson DA, Schmidt DF, Yi P, Kulanthaivel P. Application of biocatalysis to drug metabolism: preparation of mammalian metabolites of a biaryl-bis-sulfonamide AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor potentiator using Actinoplanes missouriensis. Drug Metab Dispos. 2006 Jun;34(6):925-31. Epub 2006 Feb 28.
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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.
Mibampator (LY451395) randomized clinical trial for agitation/aggression in Alzheimer's disease.[Pubmed:23257314]
Int Psychogeriatr. 2013 May;25(5):707-19.
BACKGROUND: Mibampator, an amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor potentiator, was evaluated for treatment of agitation and aggression (A/A) in Alzheimer's disease (AD). METHODS: Outpatients (n = 132) with probable AD and A/A randomized to 12 weeks of double-blind treatment with 3-mg po mibampator or placebo were assessed using the 4-domain A/A subscale of the Neuropsychiatric Inventory (NPI-4-A/A) derived from the Neuropsychiatric Inventory. Secondary measures included the Cohen-Mansfield Agitation Inventory, Cornell Scale for Depression in Dementia, Frontal Systems Behavior Inventory (FrSBe), and Alzheimer's Disease Assessment Scale-Cognitive. Efficacy was analyzed using mixed-effects model repeated measures from baseline to endpoint. Adverse events (AEs), labs, vital signs, and electrocardiograms were monitored. RESULTS: Baseline characteristics were comparable between groups. Both groups improved on the NPI-4-A/A, but without group differences. Among secondaries, mibampator was significantly better (p = 0.007) than placebo only on the FrSBe. AEs were similar between groups. One death occurred in the placebo group. CONCLUSION: Possible explanations for no significant group differences include caregiver, drug target engagement, and design issues. This trial is registered on ClinicalTrials.gov; ID: NCT00843518.
