AZD3839

製品コードS7731 バッチS773103

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H16F3N5
分子量 431.41 CAS No. 1227163-84-9
Solubility (25°C)* 体外 DMSO 86 mg/mL (199.34 mM)
Ethanol (warmed with 50ºC water bath) 86 mg/mL (199.34 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
5% dimethylacetamide 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid,pH 3
2.0mg/ml Taking the 1 mL working solution as an example, take 2 mg of this product and add it to 1 ml of 5% dimethylacetamide+20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3 clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
in vitro In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels with IC50 of 4.8 nM, and decreases the formation of sAPPβ with IC50 of 16.7 nM. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons with IC50 values of 50.9, 32.2, and 24.8 nM, respectively. [1] AZD3839 causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM. [2]
in vivo In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation. [1]

プロトコル(参考用のみ)

キナーゼアッセイ hBACE1 and hBACE2 Time-resolved-FRET Assay
The soluble part of the human β-secretase (recombinant hBACE1 enzyme, amino acids 1–460, or hBACE2 enzyme, amino acids 1–473) is mixed with compound in reaction buffer (sodium acetate, CHAPS, Triton X-100, EDTA, pH 4.5) and preincubated for 10 min. Substrate (Europium)CEVNLDAEFK(Qsy7) is added, and the reaction is allowed to proceed for 6.5 h in darkness under the lid at 22 °C until stopped with the addition of sodium acetate, pH 9. The fluorescence of the product is measured on a Victor II 1420 Multilabel Counter plate reader (Wallac) with an excitation wavelength of 340 nm and an emission wavelength of 615 nm.
動物実験 動物モデル C57BL/6 mice
投薬量 69 mg/kg daily
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] PubMed: 35253833
Identification and drug-induced reversion of molecular signatures of Alzheimer's disease onset and progression in AppNL-G-F, AppNL-F, and 3xTg-AD mouse models [ Genome Med, 2021, 13(1):168] PubMed: 34702310
Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life. [ Alzheimers Dement, 2019, 15(9):1183-1194] PubMed: 31416794
Proteolytic Processing of Neuregulin 2. [ Mol Neurobiol, 2019, 10.1007/s12035-019-01846-9] PubMed: 31838721
Elevated cleavage of neuregulin-1 by beta-secretase 1 in plasma of schizophrenia patients. [ Prog Neuropsychopharmacol Biol Psychiatry, 2019, 90:161-168] PubMed: 30500411
Increased Foxo3a Nuclear Translocation and Activity is an Early Neuronal Response to βγ-Secretase-Mediated Processing of the Amyloid-β Protein Precursor: Utility of an AβPP-GAL4 Reporter Assay. [ J Alzheimers Dis, 0, 61(2):673-688] PubMed: 29254083

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。