INDEX NAME NOT YET ASSIGNED
- CAS No.
- 2561414-56-8
- Chemical Name:
- INDEX NAME NOT YET ASSIGNED
- Synonyms
- β-cell,RIP-DTA mice,Inhibitor,insulin secretion,GNF2133,inhibit,Dual specificity tyrosine regulated kinase,glucose disposal,Dual specificity tyrosine phosphorylation regulated kinase,CD-1 mice,GNF 2133,DYRK,GNF-2133,orally active
- CBNumber:
- CB98665404
- Molecular Formula:
- C24H30N6O2
- Molecular Weight:
- 434.54
- MDL Number:
- MOL File:
- 2561414-56-8.mol
INDEX NAME NOT YET ASSIGNED Chemical Properties,Uses,Production
Biological Activity
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[1]. 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)23.5Vss (L/kg)11AUC (h.nM)326810974144420 Cmax(nM)1977167513319tmax<(h)0.033.03.0Clast(nM)36.6191324t1/2<(h)6.63.46.6F (%)22.3CD-1 mice; 30 mg/kg; p.o.sup>[1].
References
[1]. Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020 Mar 26;63(6):2958-2973.
INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials
Raw materials
Preparation Products
INDEX NAME NOT YET ASSIGNED Suppliers
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TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |
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