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YO-01027 (Synonyms: Dibenzazepine; DBZ) 纯度: 98.03%
YO-01027 (Dibenzazepine; DBZ) 是高效的 γ-分泌酶抑制剂,裂解 Notch 和 APPL 的 IC50 分别为 2.92 和 2.64 nM。
YO-01027 Chemical Structure
CAS No. : 209984-56-5
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥999 | In-stock | |
2 mg | ¥700 | In-stock | |
5 mg | ¥980 | In-stock | |
10 mg | ¥1760 | In-stock | |
25 mg | ¥3990 | In-stock | |
50 mg | 询价 | ||
100 mg | 询价 |
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YO-01027 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Neuronal Signaling Compound Library
- Stem Cell Signaling Compound Library
- Wnt/Hedgehog/Notch Compound Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Differentiation Inducing Compound Library
- Reprogramming Compound Library
- Anti-Breast Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Neurodegenerative Disease-related Compound Library
- Angiogenesis Related Compound Library
- Transcription Factor Targeted Library
- Anti-Liver Cancer Compound Library
- Anti-Colorectal Cancer Compound Library
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. |
IC50 & Target |
IC50: 2.92±0.22 (Notch), 2.64±0.30 (APPL) nM[1] |
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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[1]. The molecular targets of CE and DBZ are the N-terminal fragment of presenilin 1 within the γ-secretase complex[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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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[3]. 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[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
463.48 |
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Formula |
C26H23F2N3O3 |
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CAS 号 |
209984-56-5 |
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中文名称 |
二苯并氮卓 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 33 mg/mL (71.20 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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
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参考文献 |
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Cell Assay [1] |
DBZ (0.1, 1, 2.5, 5, 7.5, 10, 25, 50, 100, 250 nM) are added to the S2 cell medium upon induction of Notch or APPL expression, 6 h before protein harvesting. For each sample, the same inhibitor is also included at the corresponding concentration in the lysis buffer for protein extraction and immunoblot analysis[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [3] |
Mice: Male wild-type (WT) C57BL/6J and Apo E-/- mice are used in the study. Ang II-treated mice are received an intraperitoneal injection of either saline vehicle or γ-secretase inhibitor, dibenzazepine (DBZ) (1 mg/kg/d, dissolved in saline) 1 day before mini-pump implantation, and the treatment continued daily for 4 weeks. The blood pressure is measured in conscious mice using a computerized tail-cuff system. All mice are anesthetized. The aortic tissues are removed and prepared for further histological and molecular analysis[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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