Description
GNF7156 is a highly potent and selective small molecule that promotes pancreatic β cell proliferation in rodent （EC50 ~2.2 µM）and human primary islets (EC50 ~0.76 µM). It acts most likely as a result of combined inhibition of DYRK1A and GSK3B. GNF7156-treated human islets retain functionality in vitro and after transplantation into diabetic mice. Oral dosing of GNF7156 in diabetic mice induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control. Biochemical, genetic and cell biology data point to Dyrk1a as the key molecular target. GNF7156 is a good chemical tool to support the feasibility of treating diabetes with an oral therapy to restore β-cell mass, and highlights a tractable pathway for future drug discovery efforts.
Product information
CAS Number: 2041071-54-7
Molecular Weight: 418.45
Formula: C22H22N6O3
Chemical Name: 1-(3-(3-amino-6-phenylpyrazine-2-carboxamido)pyridin-4-yl)piperidine-4-carboxylic acid
Smiles: NC1=NC=C(N=C1C(=O)NC1=CN=CC=C1N1CCC(CC1)C(O)=O)C1C=CC=CC=1
InChiKey: HZCOFZVJMJRKIB-UHFFFAOYSA-N
InChi: InChI=1S/C22H22N6O3/c23-20-19(26-16(13-25-20)14-4-2-1-3-5-14)21(29)27-17-12-24-9-6-18(17)28-10-7-15(8-11-28)22(30)31/h1-6,9,12-13,15H,7-8,10-11H2,(H2,23,25)(H,27,29)(H,30,31)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
GNF7156 was used at 6.7 µM concentration in beta cell proliferation assays.
In Vivo:
GNF7156 was orally dosed to mice at 50 mg/kg twice a day for 14 days.
References:
- Shen W, et al. Inhibition of DYRK1A and GSK3B induces human β-cell proliferation. (2015) Nat Commun. 6:8372.
Products are for research use only. Not for human use.
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