aladdin 阿拉丁 I413736 Itanapraced (CHF 5074) 749269-83-8 96%

中文名：Itanapraced (CHF 5074)

英文名：Itanapraced (CHF 5074)

纯度：Moligand™，≥96%

货号：I413736

Cas号：749269-83-8

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Itanapraced (CHF 5074) Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.

Targets

γ secretase

In vitro

In human neuroglioma cells over-expressing the Swedish mutated APP [human neuroglioma cell line expressing APPswe (H4swe)], CHF5074 preferentially lowers Aβ42 secretion with an IC50 of 3.6 µmol/L. CHF5074 does not display inhibitory activity on COX-1 and COX-2 enzymes when employed at concentrations up to 100 µmol/L and 300 µmol/L respectively.

In vivo

In rats, CHF5074 is orally well absorbed (50%) and is slowly eliminated from plasma (t1/2 ≈ 20 h). In Tg2576 transgenic mice, chronic treatment with CHF5074 markedly reduces brain Aβ burden without histological signs of peripheral Notch-mediated toxicity.

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