产品
编 号：F595496
分子式：C17H11Cl2N3O2
分子量：360.19
分子式：C17H11Cl2N3O2
分子量：360.19
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2226664-93-1
产品详情
生物活性：
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
体内研究：
KY19382 (0.1 mg/kg; i.p. once daily for 2 weeks) delays growth plate senescence in older mice and promotes growth plate maturation in rapidly growing young mice.KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) significantly increases the length of tibiae in mice.KY19382 (5 mg/kg; i.p.) displays a relatively favorable bioavailability (F=16.74%), showing half-life of 16.20 h and an exposure level of 6,555.79 ng?h/ml.KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) shows reduction in adipocyte size and anti-inflammatory effects.A3051 (25 mg/kg; p.o. once daily for 5 days) reduces fasting glucose in mice.A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces the hepatosteatosis in mice.Animal Model:C57BL/6 male mice (7-weeks-old or 3-weeks-old)
Dosage:0.1 mg/kg
Administration:I.p. once daily for 2 weeks
Result:Increased nuclear β-catenin in the growth plate chondrocytes dramatically.Elevated the height of each growth plate zone and BrdU-positive cells.Did not affect the cartilage resorption of rapidly growing young mice.
Animal Model:SD male rats
Dosage:1 mg/kg for i.v. and 5 mg/kg for i.p. (Pharmacokinetic Analysis)
Administration:I.v. and i.p. administration
Result:I.v.: t1/2=3.33 h; AUC=7832.81 ng?h/mL; CL=0.12 L/h/kg.I.p.: t1/2=16.20 h; F=16.74%; Cmax=463.37 ng/mL.
体外研究：
KY19382 (0.01 and 0.1 μM; 48 h) promotes ATDC5 cells proliferation.KY19382 (0.1 μM; 3 d) up-regulates the mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells.KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β in ATDC5 cells.KY19382 (0.1 μM; 4 h) interrupts the CXXC5-DVL interaction in ATDC5 cells.KY19382 (0.001-10 μM; 18 h) enhances the TOPFlash activity in HEK293 reporter cells.KY19382 (0.1 μM; 48 h) elevates nuclear translocation of β-catenin in ATDC5 cells.
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
体内研究：
KY19382 (0.1 mg/kg; i.p. once daily for 2 weeks) delays growth plate senescence in older mice and promotes growth plate maturation in rapidly growing young mice.KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) significantly increases the length of tibiae in mice.KY19382 (5 mg/kg; i.p.) displays a relatively favorable bioavailability (F=16.74%), showing half-life of 16.20 h and an exposure level of 6,555.79 ng?h/ml.KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) shows reduction in adipocyte size and anti-inflammatory effects.A3051 (25 mg/kg; p.o. once daily for 5 days) reduces fasting glucose in mice.A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces the hepatosteatosis in mice.Animal Model:C57BL/6 male mice (7-weeks-old or 3-weeks-old)
Dosage:0.1 mg/kg
Administration:I.p. once daily for 2 weeks
Result:Increased nuclear β-catenin in the growth plate chondrocytes dramatically.Elevated the height of each growth plate zone and BrdU-positive cells.Did not affect the cartilage resorption of rapidly growing young mice.
Animal Model:SD male rats
Dosage:1 mg/kg for i.v. and 5 mg/kg for i.p. (Pharmacokinetic Analysis)
Administration:I.v. and i.p. administration
Result:I.v.: t1/2=3.33 h; AUC=7832.81 ng?h/mL; CL=0.12 L/h/kg.I.p.: t1/2=16.20 h; F=16.74%; Cmax=463.37 ng/mL.
体外研究：
KY19382 (0.01 and 0.1 μM; 48 h) promotes ATDC5 cells proliferation.KY19382 (0.1 μM; 3 d) up-regulates the mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells.KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β in ATDC5 cells.KY19382 (0.1 μM; 4 h) interrupts the CXXC5-DVL interaction in ATDC5 cells.KY19382 (0.001-10 μM; 18 h) enhances the TOPFlash activity in HEK293 reporter cells.KY19382 (0.1 μM; 48 h) elevates nuclear translocation of β-catenin in ATDC5 cells.
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