KY19382 - CAS:2226664-93-1

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KY19382 (Synonyms:A3051)

目录号 : KM6403 CAS No. : 2226664-93-1 纯度 : 98%

Data Sheet 产品使用指南

KY19382 是一种有效的和具有口服活性的 CXXC5-DVL 和 GSK3β 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。

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100mg	询价	In-stock

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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.

Cell Proliferation Assay

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

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

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.: t_1/2=3.33 h; AUC=7832.81 ng∙h/mL; CL=0.12 L/h/kg. I.p.: t_1/2=16.20 h; F=16.74%; C_max=463.37 ng/mL.

分子式

C₁₇H₁₁Cl₂N₃O₂

分子量

360.19

CAS号

2226664-93-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg	5 mg	10 mg

1 mM	2.7763 mL	13.8816 mL	27.7631 mL
5 mM	0.5553 mL	2.7763 mL	5.5526 mL
10 mM	0.2776 mL	1.3882 mL	2.7763 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： 98%

Data Sheet

产品使用指南

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