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GNF2133
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。
GNF2133图片
CAS NO:2561414-56-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
GNF2133 是一种有效的、选择性的、具有口服活性的DYRK1A抑制剂,对 DYRK1A 和 GSK3β 的IC50分别为 0.0062、>50 μM。GNF2133 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 具有研究1型糖尿病的潜力。
生物活性

GNF2133 is a potent, selective and orally activeDYRK1Ainhibitor withIC50s of 0.0062, >50 μM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increasesinsulinsecretion. GNF2133 has the potential for the research of type 1 diabetes[1].

IC50& Target[1]

DYRK1

 

DYRK1A

0.0062 μM (IC50)

GSK3β

>50 μM (IC50)

体内研究
(In Vivo)

GNF2133 (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].
GNF2133 (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 in CD-1 mice[1].

plasma (iv)plasma (po)pancreas (po)
CL (mL/min/kg)23.5//
Vss (L/kg)11//
AUC (h·nM)326810974144420
Cmax(nM)1977167513319
tmax<(h)0.033.03.0
Clast(nM)36.6191324
t1/2<(h)6.63.46.6
F (%)/22.3/
CD-1 mice; 30 mg/kg; p.o.[1].

Animal Model:CD-1 mice[1]
Dosage:30 mg/kg
Administration:P.o.
Result:Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%.
Animal Model:Wistar Han rat[1]
Dosage:30 mg/kg (0.5% methylcellulose + Tween-80)
Administration:P.o.; once a day for 5 days
Result:Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin.
Animal Model:Diphtheria toxin A (RIP-DTA) mice[1]
Dosage:3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)
Administration:P.o., once a day for 35 days
Result:Significantly improves glucose disposal capacity and increased insulin secretion.
分子量

434.53

性状

Solid

Formula

C24H30N6O2

CAS 号

2561414-56-8

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 : 4 mg/mL(9.21 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3013 mL11.5067 mL23.0134 mL
5 mM0.4603 mL2.3013 mL4.6027 mL
10 mM---------
*

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。