产品
编 号：F741654
分子式：C24H30N6O2
分子量：434.53
分子式：C24H30N6O2
分子量：434.53
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2561414-56-8
产品详情
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//
Vss (L/kg)11//
AUC (h·nM)326810974144420
Cmax(nM)1977167513319
tmax<(h)0.033.03.0
Clast(nM)36.6191324
t1/2<(h)6.63.46.6F (%)/22.3/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) 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.
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//
Vss (L/kg)11//
AUC (h·nM)326810974144420
Cmax(nM)1977167513319
tmax<(h)0.033.03.0
Clast(nM)36.6191324
t1/2<(h)6.63.46.6F (%)/22.3/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) 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.
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