Ceperognastat (LY3372689) | OGA inhibitor | Probechem Biochemicals

Chemical Structure : LY3372689

CAS No.: 2241514-56-5

加入收藏

LY3372689 (Ceperognastat, LY-3372689)

货号: PC-72902Not For Human Use, Lab Use Only.

Ceperognastat (LY3372689) is a potent, selective and CNS-penetrant, orally bioavailable O-GlcNAcase (OGA) enzyme inhibitor with SPR KD of 133 pM (human OGA), IC50 of 2.4/1.8 nM for hOGA and mOGA respectively.

规格	价格	库存
5 mg	￥2380	In stock
10 mg	￥3780	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

Ceperognastat (LY3372689) is a potent, selective and CNS-penetrant, orally bioavailable O-GlcNAcase (OGA) enzyme inhibitor with SPR KD of 133 pM (human OGA), IC50 of 2.4/1.8 nM for hOGA and mOGA respectively.

Ceperognastat (LY3372689) binds OGA from different species with high affinity (1.8-2.4 nM) and displayed no difference in binding to brain homogenates from either AD or age-matched control brains.

Ceperognastat (LY3372689) demonstrates potent inhibition of purified human and mouse OGA and is highly selective against the functionally related lysosomal hexosaminidase enzymes HexA and HexB.

Ceperognastat (LY3372689) also shows no important in vitro binding activity across an industry standard selectivity panel of receptors, ion channels, transporters, and enzymes, and exhibited weak inhibition of the human ether-à-go-go (hERG) channel.

Ceperognastat (LY3372689) induces concentration-dependent increase in O-GlcNAc modified proteins in cellular assay with EC50 of 21.9 nM.

Ceperognastat (LY3372689) shows potential therapeutic approach to reduce the spread of tau pathology and thus slow the clinical progression of AD.

物理化学性质&存储条件

分子量	383.442
分子式	C16H22FN5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-fluoro-5-(((2S,4S)-2-methyl-4-((5-methyl-1,2,4-oxadiazol-3-yl)methoxy)piperidin-1-yl)methyl)thiazol-2-yl)acetamide

参考文献

1. Patent WO2018140299A1.
2. Kielbasa W, et al. Alzheimers Dement (N Y). 2024 Dec 26;10(4):e70020.

LY3372689 (Ceperognastat, LY-3372689)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

LY3372689 (Ceperognastat, LY-3372689)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.