Flurizan - CAS 51543-40-9
Catalog number:
51543-40-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C15H13FO2
Molecular Weight:
244.26
COA:
Inquire
Targets:
γ-secretase
Description:
Flurizan, also called Tarenflurbil, is a nonsteroidal anti-inflammatory drug which inhibits γ-secretase activity leading to preventing the formation of the amyloid β peptide (Aβ42) from amyloid β precursor protein (APP).
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Brife Description:
Reduces Aβ42 levels (Amyloid-β: IC50 = 280 µM (human); γ-secretase inhibitor
Appearance:
White solid
Synonyms:
(2R)-2-(3-fluoro-4-phenylphenyl)propanoic acid; 257-264-7; 501W00OOWA; flurizan; MPC-7869; MPC7869; tarenflurbil; Tarenflurbil; (R)-Flurbiprofen; Flurizan; R-Flurbiprofen; 51543-40-9; (R)-2-Flurbiprofen; MPC-7869; (2R)-2-(3-fluoro-4-phenylphenyl)propanoic acid; (R)-2-Flubiprofen; (2r)-2-(3-Fluoro-4-Phenyl-Phenyl)propanoic Acid; UNII-501W00OOWA; (-)-(2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid; CHEMBL190083; CHEBI:38666; (2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid; E-7869; (R)-(-)-2-Fluoro-alpha-methyl-4-biphenylacetic acid; (R)-2-Fluoro-alpha-methyl(1,1'-biphenyl)-4-acetic acid; Flurwood; (2R)-2-(2-fluoro-[1,1'-biphenyl-4-yl])propanoic acid; Urbifen, Ansaid, Flurwood, Froben, Flurbiprofen; Furbiprofen; TruNoc; NSC685699; NCGC00016654-01; (-)-Flurbiprofen; FLP; CAS-5104-49-4; S1679_Selleck; Tocris-1769;
Solubility:
Soluble to 49 mM at 25ºC in DMSO, to 49 mM at 25ºC in ethanol, to <1 mM at 25ºC in water, to ~25 mM in DMF, and to ~0.9 mM in PBS (pH 7.2).
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -31℃ for long term (months to years).
MSDS:
Inquire
Boiling Point:
162.4℃ at 760 mmHg
Melting Point:
110-113℃
Density:
1.555 g/cm3
InChIKey:
SYTBZMRGLBWNTM-SNVBAGLBSA-N
InChI:
1S/C15H13FO2/c1-10(15(17)18)12-7-8-13(14(16)9-12)11-5-3-2-4-6-11/h2-10H,1H3,(H,17,18)/t10-/m1/s1
Canonical SMILES:
CC(C1=CC(=C(C=C1)C2=CC=CC=C2)F)C(=O)O
Current Developer:
γ-secretase
1.Generalized model of electromigration with 1:1 (analyte:selector) complexation stoichiometry: part II. Application to dual systems and experimental verification.
Müllerová L1, Dubský P2, Gaš B1. J Chromatogr A. 2015 Mar 6;1384:147-54. doi: 10.1016/j.chroma.2015.01.055. Epub 2015 Jan 23.
Interactions among analyte forms that undergo simultaneous dissociation/protonation and complexation with multiple selectors take the shape of a highly interconnected multi-equilibrium scheme. This makes it difficult to express the effective mobility of the analyte in these systems, which are often encountered in electrophoretical separations, unless a generalized model is introduced. In the first part of this series, we presented the theory of electromigration of a multivalent weakly acidic/basic/amphoteric analyte undergoing complexation with a mixture of an arbitrary number of selectors. In this work we demonstrate the validity of this concept experimentally. The theory leads to three useful perspectives, each of which is closely related to the one originally formulated for simpler systems. If pH, IS and the selector mixture composition are all kept constant, the system is treated as if only a single analyte form interacted with a single selector.
2.Novel flurbiprofen derivatives with improved brain delivery: synthesis, in vitro and in vivo evaluations.
Zheng D1, Shuai X, Li Y, Zhou P, Gong T, Sun X, Zhang Z. Drug Deliv. 2015 Jul 21:1-10. [Epub ahead of print]
Tarenflurbil (R-flurbiprofen) was acknowledged as a promising candidate in Alzheimer's disease (AD) therapy. However, the Phase III study of tarenflurbil was extremely restricted by its poor delivery efficiency to the brain. To tackle this problem, the novel carriers for tarenflurbil, racemic flurbiprofen (FLU) derivatives (FLU-D1 and FLU-D2) modified by N,N-dimethylethanolamine-related structures were synthesized and characterized. These derivatives showed good safety level in vitro and they possessed much higher cellular uptake efficiency in brain endothelial cells than FLU did. More importantly, the uptake experiments suggested that they were internalized via active transport mechanisms. Biodistribution studies in rats also illustrated a remarkably enhanced accumulation of these derivatives in the brain. FLU-D2, the ester linkage form of these derivatives, achieved a higher brain-targeting efficiency. Its Cmax and AUC0-t were enhanced by 12.
3.γ-Secretase modulator in Alzheimer's disease: shifting the end.
Xia W1, Wong ST, Hanlon E, Morin P. J Alzheimers Dis. 2012;31(4):685-96. doi: 10.3233/JAD-2012-120751.
The outcomes of the clinical trials of the γ-secretase inhibitor Semagacestat (LY-450139) and the γ-secretase modulator (GSM) Tarenflurbil were disappointing, but may not represent the end of the γ-secretase era. γ-Secretase modulators, by definition, only block the γ-secretase cleavage of amyloid-β protein precursor (AβPP) to generate the longer, 42-residue amyloid-β (Aβ42) without changing the production of total Aβ. The first generation GSMs were shown to block Aβ42 generation while increasing Aβ38. The non-steroidal anti-inflammatory drug, Tarenflurbil, binds to AβPP and shifts the cleavage site from Aβ42 to Aβ38. In addition, Tarenflurbil does not affect the γ-secretase cleavage of Notch. Even before the failed clinical trials of Tarenflurbil, second generation GSMs had emerged, and some of these GSMs interact with presenilin, which carries the active site of the γ-secretase. While second generation GSMs are pharmacologically superior to first generation GSMs, in vivo Aβ profiles (decreased levels of Aβ38, Aβ40, and Aβ42) in animals treated with potent GSMs are strikingly different from those in cultured cells.
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