BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins.
| Molecular Weight | 496.42 |
| Formula | C24H16F4N6O2 |
| CAS Number | 1799753-84-6 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Qin Wu, et al. GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer
| Related GLUT Products |
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| GLUT inhibitor-1
GLUT inhibitor-1 is a potent and orally active glucose transporter protein (GLUT) inhibitor that targets GLUT1 and GLUT3 with IC50 values of 242 nM and 179 nM, respectively.GLUT inhibitor-1 can be used in cancer and autoimmune disease related studies. |
| SLC26A3-IN-3
SLC26A3-IN-3 is a SLC26A3 inhibitor (IC50: 40 nM). |
| MSNBA
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. |
| SLC26A3-IN-1
SLC26A3-IN-1 is an inhibitor of anion exchanger protein SLC26A3 (IC50=340 nM). |
| SLC26A3-IN-2
SLC26A3-IN-2 is an orally active inhibitor of anion exchanger protein SLC26A3 (IC50=360 nM). |
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