GNF7156, β Cell Proliferation Inducer


Catalog No. size PriceQuantity
M60293-2S 2 mg solid $139
M60293-10S 10mg solid $556

Description

Product Information
Molecular Weight: 418.45
Formula: C22H22N6O3
Purity: ≥ 98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: 1-(3-(3-amino-6-phenylpyrazine-2-carboxamido)pyridin-4-yl)piperidine-4-carboxylic acid
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

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.

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.

Reference:

  • 1. 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. 

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed