YO-01027 (Dibenzazepine, DBZ)|209984-56-5|(Dibenzazepine; DBZ)-陌孚医药/Medlife

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YO-01027 (Dibenzazepine, DBZ) (Synonyms: Dibenzazepine; DBZ)

目录号: PC15649 纯度: ≥98%

CAS No. :209984-56-5

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PC15649-5mg	5mg	¥1009.40	请登录
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PC15649-25mg	25mg	¥3714.20	请登录
PC15649-50mg	50mg	¥5497.80	请登录
PC15649-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥980.00	请登录

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中文名称

YO-01027 (Dibenzazepine, DBZ)

中文别名

N-((1S)-2-(((7S)-6,7-二氢-5-甲基-6-氧代-5H-二苯并(b,d)氮杂卓-7-基)氨基)-1-甲基-2-氧代乙基)-3,5-二氟苯乙酰胺;N-[(1S)-2-[[(7S)-6,7-二氢-5-甲基-6-氧代-5H-二苯并[B,D]氮杂卓-7-基]氨基]-1-甲基-2-氧代乙基]-3,5-二氟苯乙酰胺;YO-01027 (Dibenzazepine) 抑制剂;YO-01027-分泌酶抑制剂;γ-分泌酶抑制剂;叔丁基2-氨基乙基(乙基)氨基甲酸酯;环维黄杨星D

英文名称

YO-01027 (Dibenzazepine, DBZ)

英文别名

(S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanamide;YO-01027;(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide;DBZ;DIBENZAZEPINE;Dibenzazepine (Deshydroxy LY 411575);N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-Benzeneacetamide;YO01027;YO-01027 (Dibenzazepine);Dibenzazepine (deshydroxy LY 411575) DBZ;Deshydroxy LY-411575;LY411575;N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide;γ-Secretase inhibitor XX;(S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide;GSI-XX;gamma-Secretase Inhibitor XX;Deshydroxy LY 411575;(S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5;N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoroben

Cas No.

209984-56-5

分子式

C₂₆H₂₃F₂N₃O₃

分子量

463.48

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC₅₀ values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM

体外研究(In Vitro)

Increasing concentrations of DBZ administered to APPL- or Notch-expressing cells leads to the progressive accumulation of APPL CTF fragments and a decrease in NICD production in a strictly dose-dependent manner. The molecular targets of CE and DBZ are the N-terminal fragment of presenilin 1 within the γ-secretase complex.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

DBZ blocks activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E mice and human undergoing AAA repair. DBZ markedly prevents Ang II-stimulated accumulation of macrophages and CD4+ T cells, and ERK-mediated angiogenesis, simultaneously reverses Th2 response, in vivo. Administration of DBZ markedly attenuates renal fibrosis and expression of fibrotic markers, including collagen 1α1/3α1, fibronectin, and α-smoothmuscle actin. DBZ significantly inhibits ureteral obstruction -induced expression of transforming growth factor (TGF)- β, phosphorylated Smad 2, and Smad 3.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Groth C, et al. Pharmacological analysis of Drosophila melanogaster gamma-secretase with respect to differential proteolysis of Notch and APP. Mol Pharmacol. 2010 Apr;77(4):567-74. [Information]

[2]. Fuwa H, et al. Divergent synthesis of multifunctional molecular probes to elucidate the enzyme specificity of dipeptidic gamma-secretase inhibitors. ACS Chem Biol. 2007 Jun 15;2(6):408-18. [Information]

[3]. Zheng YH, et al. Notch γ-secretase inhibitor dibenzazepine attenuates angiotensin II-induced abdominal aortic aneurysm in ApoE knockout mice by multiple mechanisms. PLoS One. 2013 Dec 16;8(12):e83310. [Information]

[4]. Xiao Z, et al. The Notch γ-secretase inhibitor ameliorates kidney fibrosis via inhibition of TGF-β/Smad2/3 signaling pathway activation. Int J Biochem Cell Biol. 2014 Oct;55:65-71. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (107.88 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1576 mL	10.7880 mL	21.5759 mL
5 mM	0.4315 mL	2.1576 mL	4.3152 mL
10 mM	0.2158 mL	1.0788 mL	2.1576 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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