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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。

  • 货号:
    TK0467
  • 规格:
    2mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

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%