顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷

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产品名称:顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸

CAS:471905-41-6

别名：顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸;顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸,一种适度有效的Γ-SECRETASE(Γ-分泌酶)抑制剂

英文名：cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid

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生物活性MK-0752是一种适度有效的γ-secretase（γ-分泌酶）抑制剂，降低Aβ40产量，IC50为5 nM。Phase 1/2。
体外研究MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation.
体内研究MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain.
特征MK-0752 is a moderately potent γ-secretase inhibitor.