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KY19382
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KY19382图片
CAS NO:2226664-93-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
A3051
产品介绍
KY19382 是一种有效的和具有口服活性的CXXC5-DVLGSK3β的双重抑制剂,IC50值分别为 19 和 10 nM。KY19382 通过对 CXXC5-DVL 相互作用和 GSK3β 活性的抑制作用激活 Wnt/β-catenin 信号传导。KY19382 可用于高脂饮食 (HFD) 诱发的代谢性疾病的研究。
生物活性

KY19382 is a potent and orally active dual inhibitor ofCXXC5-DVLandGSK3β, withIC50s 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[1][2].

IC50& Target[1]

CXXC5-DVL

19 nM (IC50)

GSK3β

10 nM (IC50)

体外研究
(In Vitro)

KY19382 (0.01 and 0.1 μM; 48 h) promotes ATDC5 cells proliferation[1].
KY19382 (0.1 μM; 3 d) up-regulates the mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells[1].
KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β in ATDC5 cells[1].
KY19382 (0.1 μM; 4 h) interrupts the CXXC5-DVL interaction in ATDC5 cells[1].
KY19382 (0.001-10 μM; 18 h) enhances the TOPFlash activity in HEK293 reporter cells[1].
KY19382 (0.1 μM; 48 h) elevates nuclear translocation of β-catenin in ATDC5 cells[1].

Cell Proliferation Assay[1]

Cell Line:ATDC5 cells
Concentration:0, 0.01, 0.1 μM
Incubation Time:48 hours
Result:Enhanced the number of BrdU-positive ATDC5 cells.

Cell Proliferation Assay[1]

Cell Line:ATDC5 cells
Concentration:0, 0.01, 0.1 μM
Incubation Time:24 hours
Result:Increased the level of β-catenin in a dose-dependent manner.
体内研究
(In Vivo)

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[1].
KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) significantly increases the length of tibiae in mice[1].
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 ngoh/ml[1].
KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) shows reduction in adipocyte size and anti-inflammatory effects[2].
A3051 (25 mg/kg; p.o. once daily for 5 days) reduces fasting glucose in mice[2].
A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces the hepatosteatosis in mice[2].

Animal Model:C57BL/6 male mice (7-weeks-old or 3-weeks-old)[1]
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[1]
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.
分子量

360.19

性状

Solid

Formula

C17H11Cl2N3O2

CAS 号

2226664-93-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL(13.88 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7763 mL13.8816 mL27.7631 mL
5 mM0.5553 mL2.7763 mL5.5526 mL
10 mM0.2776 mL1.3882 mL2.7763 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。