Description
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
InChiKey: KBKQTKIWWDIVTN-HQCIMWSJSA-N
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.
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