GKA50 quarterhydrate

Catalog No. Size PriceQuantity
M13641-2 Contact sales@xcessbio.com for quotation $100


GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.

Product information

Molecular Weight: 469.01

Formula: C104H114N8O25

Chemical Name: tetrakis(6-(3-{[(2S)-1-methoxypropan-2-yl]oxy}-5-{[(2S)-1-phenylpropan-2-yl]oxy}benzamido)pyridine-3-carboxylic acid) hydrate

Smiles: O.C[C@@H](CC1C=CC=CC=1)OC1=CC(=CC(=C1)C(=O)NC1=CC=C(C=N1)C(O)=O)O[C@@H](C)COC.C[C@@H](CC1C=CC=CC=1)OC1=CC(=CC(=C1)C(=O)NC1=CC=C(C=N1)C(O)=O)O[C@@H](C)COC.C[C@@H](CC1C=CC=CC=1)OC1=CC(=CC(=C1)C(=O)NC1=CC=C(C=N1)C(O)=O)O[C@@H](C)COC.C[C@@H](CC1C=CC=CC=1)OC1=CC(=CC(=C1)C(=O)NC1=CC=C(C=N1)C(O)=O)O[C@@H](C)COC


InChi: InChI=1S/4C26H28N2O6.H2O/c4*1-17(11-19-7-5-4-6-8-19)33-22-12-21(13-23(14-22)34-18(2)16-32-3)25(29)28-24-10-9-20(15-27-24)26(30)31;/h4*4-10,12-15,17-18H,11,16H2,1-3H3,(H,30,31)(H,27,28,29);1H2/t4*17-,18-;/m0000./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 46 mg/mL (98.08 mM; Need ultrasonic and warming).

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:

GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50 values ranging from 1 to 2 μM. GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells. GKA50 activates human glucokinase enzymatic activity with an EC50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC50 of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD.

In Vivo:

GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal 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