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AZD3839 Sale

目录号 : GC14130

An inhibitor of BACE1

AZD3839 Chemical Structure

Cas No.:1227163-84-9

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5mg
¥977.00
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10mg
¥1,491.00
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50mg
¥4,925.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Description:

IC50: 16.7 nM for BACE1

β-Site amyloid precursor protein cleaving enzyme1 (BACE1) is one of the key enzymes involved in the processes of the amyloid precursor protein (APP) and formation of amyloid β peptide (Aβ) species. Because cerebral deposition of Aβ species is possibly critical for the pathogenesis of Alzheimer disease, BACE1 has emerged as a key target for the treatment of this disease. AZD3839 is a potent and selective BACE1 inhibitor.

In vitro: AZD3839 concentration-dependently inhibited BACE1 activity in a biochemical fluorescence resonance energy transfer assay, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from guinea pig and mouse primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively [1].

In vivo: AZD3839 exhibited dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. PK/PD analyses of mouse and guinea pig data showed a good correlation between the potency of AZD3839 in primary cortical neurons and in vivo brain effects [1].

Clinical trial: Based on the pharmacological profile and its drug like properties, AZD3839 has been progressed into Phase 1 clinical trials in man [2].

Reference:
[1] Jeppsson F, Eketj?ll S, Janson J, Karlstr?m S, Gustavsson S, Olsson LL, Rades?ter AC, Ploeger B, Cebers G, Kolmodin K, Swahn BM, von Berg S, Bueters T, F?lting J.  Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem. 2012 Nov 30;287(49):41245-57.
[2] https://clinicaltrials. gov/ct2/show/NCT01348737?term=AZD3839&rank=1

Chemical Properties

Cas No. 1227163-84-9 SDF
化学名 (S)-3-(2-(difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)isoindolin-1-imine
Canonical SMILES FC1=CC=CC([C@@]2(C3=CC(C(F)F)=NC=C3)C4=CC=CC(C5=CN=CN=C5)=C4)=C1C(N2)=N
分子式 C24H16F3N5 分子量 431.41
溶解度 DMF: 2 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.318 mL 11.5899 mL 23.1798 mL
5 mM 0.4636 mL 2.318 mL 4.636 mL
10 mM 0.2318 mL 1.159 mL 2.318 mL
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