PF-06751979

Name: PF-06751979
Brand: TargetMol
SKU: T12429
Rating: 4.5 (1 reviews)

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产品编号 T12429Cas号 1818339-66-0

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

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产品编号 T12429Cas号 1818339-66-0

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

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产品介绍

生物活性

产品描述	PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
靶点活性	BACE2:194 nM , BACE1:7.3 nM
体外活性	PF-06751979 shows improved selectivity over BACE2 (IC50=194 nM) in binding (27-fold) relative to the literature examples and across multiple chemical series in BACE1 program.
体内活性	PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2. Acute administration of PF-06751979 yields a robust dose-responsive and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40 with peak inhibition at 3 h of >77%.[1].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: 50 mg/mL (109.77 mM), Sonication is recommended.

DMSO: 150 mg/mL (329.31 mM), Sonication is recommended.

溶液配制表

Ethanol/DMSO