GNF2133

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GNF2133 是一种有效的选择性 DYRK1A 抑制剂，IC50 为 6.2 nM。 GNF2133 可用于有关 1 型糖尿病的研究。

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.(In Vitro):GNF2133 has an IC50 of >50 μM for GSK3β. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion.(In Vivo):In Diphtheria toxin A (RIP-DTA) mice, GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion. In CD-1 mice, GNF2133 (30 mg/kg; p.o.) shows moderate plasma exposure and good oral absorption with oral bioavailability of 22.3%. In Wistar Han rat, GNF2133 (30 mg/kg; p.o.) increases in cell proliferation marker Ki67 and insulin and reduces cyclin D1 levels and overall cell density.

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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.CD-1 mice; 30 mg/kg; p.o.. 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) miceDosage:3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)Administration:P.o., once a day for 35 daysResult:Significantly improves glucose disposal capacity and increased insulin secretion.

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Others

Other Targets

VEGFR|Tyrosine Kinases

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2561414-56-8

434.53

C24H30N6O2

>98% (HPLC)

In Vitro:?DMSO : 4 mg/mL (9.21 mM)

O=C(NC1=NC=CC(=C1)C2=CN(C=3C=NC=CC23)C4CCOCC4)N5CCN(CC)CC5

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(-20℃)

With Ice Pack

≥ 2 years