5074,00 CHF

5074,00 CHF

CAT N°: 27917
Price:

From €55.00 €46.75

CHF5074 is a modulator of ?-secretase and a derivative of flurbiprofen (Item No. 70250).{51052} It inhibits the secretion of amyloid ? (1-42) (A?42) in H4-APP695NL human neuroglioma cells that overexpress a mutated form of amyloid precursor protein (APP; IC50 = 41 µM) and selectively inhibits secretion of A?42 over A?40 with 79% and 14% inhibition, respectively, at 100 µM. It does not inhibit COX-1 or COX-2 when used at concentrations up to 100 and 500 µM, respectively, and does not induce Notch cleavage in HEK293 cells expressing the APP mutant APPswe at 5 µM.{51052,51053} CHF5074 decreases plasma levels of A?42 in the Tg2576 transgenic mouse model of Alzheimer’s disease when administered at a dose of 12.5 mg/kg per day for seven days and reduces the plaque area and number of plaques in the brain of hAPP mice when administered in the diet at 375 ppm for six months.{51052,35877} It decreases the distance traveled, but not the escape latency, in the Morris water maze in hAPP mice compared to hAPP animals administered a vehicle control.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-(3′,4′-dichloro-2-fluoro[1,1′-biphenyl]-4-yl)-cyclopropanecarboxylic acid
  • Correlated keywords
    • A?-42-40 H4APP695NL H4-APP-695-NL COX1 COX2 HEK-293 Tg-2576 APP-swe CS-1103 CS1103
  • Product Overview:
    CHF5074 is a modulator of ?-secretase and a derivative of flurbiprofen (Item No. 70250).{51052} It inhibits the secretion of amyloid ? (1-42) (A?42) in H4-APP695NL human neuroglioma cells that overexpress a mutated form of amyloid precursor protein (APP; IC50 = 41 µM) and selectively inhibits secretion of A?42 over A?40 with 79% and 14% inhibition, respectively, at 100 µM. It does not inhibit COX-1 or COX-2 when used at concentrations up to 100 and 500 µM, respectively, and does not induce Notch cleavage in HEK293 cells expressing the APP mutant APPswe at 5 µM.{51052,51053} CHF5074 decreases plasma levels of A?42 in the Tg2576 transgenic mouse model of Alzheimer’s disease when administered at a dose of 12.5 mg/kg per day for seven days and reduces the plaque area and number of plaques in the brain of hAPP mice when administered in the diet at 375 ppm for six months.{51052,35877} It decreases the distance traveled, but not the escape latency, in the Morris water maze in hAPP mice compared to hAPP animals administered a vehicle control.

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