KY-02327

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KY-02327 是一种口服活性小分子 Disheveled (Dvl)-CXXC5 相互作用抑制剂，IC50 为 3.1 uM。

KY-02327 is an orally active, small molecule inhibitor of the Dishevelled (Dvl)-CXXC5 interaction with IC50 of 3.1 uM, a metabolically stabilized KY-02061 analog; KY-02327 is more stable by 2.3-fold and 1.3-fold than KY-02061 in rat liver microsomes and in human hepatocytes, respectively; shows enhanced effect on induction of ALP activity of osteoblast cells compared with KY-02061; activates the Wnt/β-catenin pathway, promotes osteoblast differentiation, and rescues BMD, bone volume, and trabecular bone structures in variectomized (OVX) mouse model.

KY-02327 (1-10 μM; 2 days; MC3T3E1 cells, a murine pre-osteoblast cell line) increases β-catenin protein level together with Runx2 and accumulated nuclear β-catenin in a dose-dependent manner.KY-02327 (1-10 μM) increases the mRNA levels of osteoblast differentiation markers collagen 1a (Col1a) and osteocalcin (OCN). T

KY-02327 (20 mg/kg; p.o.; 5 sequential days per week for 4 weeks) successfully rescues bone loss in the ovariectomized (OVX) mouse model. Animal Model:8-week-old female BL6 mice (ovariectomized (OVX)-induced osteoporosis model mice)Dosage:20 mg/kg Administration:P.o.; administered for 5 sequential days per week for 4 weeks Result:Newly formed bones which labeled with calcein were decreased in the femur of vehicle‐treated OVX mice.

KY02327

Wnt/Notch/Hedgehog

Dishevelled

Dishevelled

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2093407-25-9

373.453

C20H27N3O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (267.77 mM)

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ethyl 5-hydroxy-1-(2-oxo-2-((2-(piperidin-1-yl)ethyl)amino)ethyl)-1H-indole-2-carboxylate

(-20℃)

With Ice Pack

≥ 2 years