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GNF2133 hydrochloride , CAS No.2561414-57-9

COA

Cas Number: 2561414-57-9
Molecular Weight: 470.99

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Item Number

G647518

Grouped product items
SKU	Size	Availability	Price	Qty
G647518-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$480.90
G647518-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$780.90

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Basic Description

Biochemical and Physiological Mechanisms	GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC 50 s 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
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC 50 s 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 In Vivo 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 IC50& Target:DYRK1A 0.0062 μM (IC 50 ) GSK3β >50 μM (IC 50 )

Names and Identifiers

Smiles	O=C(N1CCN(CC1)CC)NC2=NC=CC(C3=CN(C4CCOCC4)C5=C3C=CN=C5)=C2.Cl
Molecular Weight	470.99

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