GNF2133|cas:2561414-56-8|西域试剂

GNF2133,98.49%

产品编号：Bellancom-142295| CAS NO：2561414-56-8| 分子式：C₂₄H₃₀N₆O₂| 分子量：434.53

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-142295		￥4800.00	杭州北京（现货）
Bellancom-142295		￥7800.00	杭州北京（现货）

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GNF2133

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 active DYRK1A inhibitor with IC₅₀s 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 increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.

体外研究

体内研究

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

	plasma (iv)	plasma (po)	pancreas (po)
CL (mL/min/kg)	23.5	/	/
V_{ss (L/kg)}	11	/	/
AUC (h·nM)	3268	10974	144420
C_max(nM)	1977	1675	13319
t_max<(h)	0.03	3.0	3.0
C_last(nM)	36.6	19	1324
t_1/2<(h)	6.6	3.4	6.6
F (%)	/	22.3	/

CD-1 mice; 30 mg/kg; p.o..

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CD-1 mice
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
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
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.

体内研究

	plasma (iv)	plasma (po)	pancreas (po)
CL (mL/min/kg)	23.5	/	/
V_{ss (L/kg)}	11	/	/
AUC (h·nM)	3268	10974	144420
C_max(nM)	1977	1675	13319
t_max<(h)	0.03	3.0	3.0
C_last(nM)	36.6	19	1324
t_1/2<(h)	6.6	3.4	6.6
F (%)	/	22.3	/

CD-1 mice; 30 mg/kg; p.o..

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CD-1 mice
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
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
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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3013 mL	11.5067 mL	23.0134 mL
5 mM	0.4603 mL	2.3013 mL	4.6027 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°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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式