YO-01027 (Dibenzazepine, DBZ) 二苯并氮卓
DBZ (Dibenzazepine)是一种二肽γ-secretase抑制剂,作用于APPL和Notch分裂, 无细胞试验中IC50分别为2.6 nM和2.9 nM。
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货号:
TK0467 -
规格:
- 2mg
- 5mg
- 10mg
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价格:
¥0.00
DBZ (Dibenzazepine)是一种二肽γ-secretase抑制剂,作用于APPL和Notch分裂, 无细胞试验中IC50分别为2.6 nM和2.9 nM。
| CAS No. | 209984-56-5 |
| 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. |
| 分子式 | C26H23F2N3O3 |
| 分子量 | 463.48 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder, -20°C ,3 years |
| 溶解性数据 | DMSO : ≥ 33 mg/mL (71.20 mM),H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
| 体内研究 | 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. |
| 体外研究 | 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. |
| 纯度及产品资料 | 98% |