AK-7

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、脑渗透性 SIRT2 抑制剂，IC50 为 15.5 uM。

A potent, selective and brain-permeable SIRT2 inhibitor with IC50 of 15.5 uM; reduces cholesterol in cultured naive neuronal cells and brain slices from wild-type mice; shows neuroprotective activity in Huntington's disease mouse models, and reduces cholesterol in neuronal models.

AK-7 (10 μM) reduces cholesterol levels in naive N2a neuroblastoma cells and hippocampal slice cultures from wild-type mice. AK-7 (1 μM) shows neuroprotective effect of AK-7 in striatal Huntington’s disease (HD) neurons. AK-7 (12.5 μM) decreases ratio of DA neurons in primary midbrain cultures.

AK-7 (15 mg/kg/dose, i.p.) is brain-permeable in wild-type and HD mice. AK-7 (10, 20 mg/kg, i.p.) improves the behavior and neuropathological phenotype and extends survival of R6/2 HD mice. AK-7 (20 mg/kg) ameliorates HD neuropathology in R6/2 mice. AK-7 also reduces the polyglutamine aggregation in R6/2 brain. In addition, AK-7 treated 140CAG mice show motor performance changes that parallel untreated wild-type mice, with the 20 mg/kg dose being most effective and significantly different from untreated 140CAG mice.

AK 7 | AK7

Chromatin/Epigenetic

Sirtuin

Sirtuin

Neurological Disease

——

420831-40-9

437.3506

C19H21BrN2O3S

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC=CC(Br)=C1)C2=CC=CC(S(=O)(N3CCCCCC3)=O)=C2

Benzamide, N-(3-bromophenyl)-3-[(hexahydro-1H-azepin-1-yl)sulfonyl]-

(-20℃)

With Ice Pack

≥ 2 years