GNF2133 hydrochloride|cas:2561414-57-9|西域试剂

GNF2133 hydrochloride

产品编号：Bellancom-142295A| CAS NO：2561414-57-9| 分子式：C₂₄H₃₁ClN₆O₂| 分子量：470.99

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

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GNF2133 hydrochloride

产品介绍

GNF2133 hydrochloride 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 hydrochloride 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 hydrochloride 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 hydrochloride 具有研究1型糖尿病的潜力。

生物活性

GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC₅₀s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.

体外研究

体内研究

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