GKA 50
Modify Date: 2024-01-12 10:03:00
GKA 50 structure
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Common Name | GKA 50 | ||
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| CAS Number | 851884-87-2 | Molecular Weight | 464.51000 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H28N2O6 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of GKA 50GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats[1][2]. |
| Name | 6-[(3-{[(2S)-1-Methoxy-2-propanyl]oxy}-5-{[(2S)-1-phenyl-2-propan yl]oxy}benzoyl)amino]nicotinic acid |
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| Description | GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats[1][2]. |
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| Related Catalog | |
| In Vitro | GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50values ranging from 1 to 2 μM[2]. GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells[2]. 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[2]. Cell Proliferation Assay[2] Cell Line: INS-1 cells (starved overnight with 3 μM glucose) Concentration: 0.01-100 μM Incubation Time: 24 hours Result: Stimulated cell proliferation in a dose-dependent manner, with EC50 values ranging from 1 to 2 μM. |
| In Vivo | GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test[1]. Animal Model: High-fat-fed obese female Zucker (fa/fa) rats[1] Dosage: 1, 3, 10, 30 mg/kg Administration: Oral administration Result: Significant percentage glucose lowering. |
| References |
| Molecular Formula | C26H28N2O6 |
|---|---|
| Molecular Weight | 464.51000 |
| Exact Mass | 464.19500 |
| PSA | 110.47000 |
| LogP | 4.83980 |