WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319792
CAS#: 375345-95-2
Description: Mibampator, also known as LY-451395, is an AMPA receptor potentiator under development for agitation/aggression in Alzheimer's disease. Patients treated with LY451395 did not show a statistically significant separation from patients taking placebo on the Alzheimer's Disease Assessment Scale-Cognitive Subscale, the primary outcome measure.
Hodoodo Cat#: H319792
Name: Mibampator
CAS#: 375345-95-2
Chemical Formula: C21H30N2O4S2
Exact Mass: 438.16
Molecular Weight: 438.601
Elemental Analysis: C, 57.51; H, 6.89; N, 6.39; O, 14.59; S, 14.62
Synonym: LY-451395; LY 451395; LY451395; Mibampator
IUPAC/Chemical Name: (R)-N-(2-(4'-(2-(methylsulfonamido)ethyl)-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonamide
InChi Key: ULRDYYKSPCRXAJ-KRWDZBQOSA-N
InChi Code: 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
SMILES Code: CC(S(=O)(NC[C@@H](C1=CC=C(C2=CC=C(CCNS(=O)(C)=O)C=C2)C=C1)C)=O)C
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, not in water
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 438.60 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Kiss T, Feng J, Hoffmann WE, Shaffer CL, Hajós M. Rhythmic theta and delta activity of cortical and hippocampal neuronal networks in genetically or pharmacologically induced N-methyl-D-aspartate receptor hypofunction under urethane anesthesia. Neuroscience. 2013 May 1;237:255-67. doi: 10.1016/j.neuroscience.2013.01.058. Epub 2013 Feb 8. PubMed PMID: 23396086.
2: Ballard C, Francis P, Corbett A. Randomized controlled trial of mibampator for behavioral and psychological symptoms of dementia: comments on the trial and thoughts for future studies. Int Psychogeriatr. 2013 May;25(5):687-9. doi: 10.1017/S1041610213000033. Epub 2013 Jan 25. PubMed PMID: 23347752.
3: Trzepacz PT, Cummings J, Konechnik T, Forrester TD, Chang C, Dennehy EB, Willis BA, Shuler C, Tabas LB, Lyketsos C. Mibampator (LY451395) randomized clinical trial for agitation/aggression in Alzheimer's disease. Int Psychogeriatr. 2013 May;25(5):707-19. doi: 10.1017/S1041610212002141. Epub 2012 Dec 21. PubMed PMID: 23257314; PubMed Central PMCID: PMC3938603.
4: Malá H, Chen Y, Worm VH, Kure J, Kaae BH, Madsen U, Badolo L, Pickering DS, Mogensen J. Cognitive enhancing effects of an AMPA receptor positive modulator on place learning in mice. Behav Brain Res. 2012 Jan 1;226(1):18-25. doi: 10.1016/j.bbr.2011.08.036. Epub 2011 Sep 1. PubMed PMID: 21906629.
5: Kiss T, Hoffmann WE, Hajós M. Delta oscillation and short-term plasticity in the rat medial prefrontal cortex: modelling NMDA hypofunction of schizophrenia. Int J Neuropsychopharmacol. 2011 Feb;14(1):29-42. doi: 10.1017/S1461145710000271. Epub 2010 Mar 25. PubMed PMID: 20334724.
6: Jones N, 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. PubMed PMID: 17851540.
7: O'Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson's disease. Curr Drug Targets. 2007 May;8(5):603-20. Review. PubMed PMID: 17504104.
8: Chappell AS, Gonzales C, Williams J, Witte MM, Mohs RC, Sperling R. AMPA potentiator treatment of cognitive deficits in Alzheimer disease. Neurology. 2007 Mar 27;68(13):1008-12. PubMed PMID: 17389305.
9: Jhee SS, Chappell AS, Zarotsky V, Moran SV, Rosenthal M, Kim E, Chalon S, Toublanc N, Brandt J, Coutant DE, Ereshefsky L. 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. PubMed PMID: 16554450.
10: Zmijewski M, 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. PubMed PMID: 16507647.
