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Inhibitory effects against the organic cation transporter 2-mediated uptake of [14C]metformin by PF-04971729 also were very weak (IC50 900μM).The disposition of PF-04971729, an orally active selective inhibitor of the sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [14C]-PF-04971729 to healthy human subjects. The absorption of PF-04971729 in humans was rapid with a Tmax at ~ 1.0 h. Of the total radioactivity excreted in feces and urine, unchanged PF-04971729 collectively accounted for ~ 35.3% of the dose, suggestive of moderate metabolic elimination in humans.
| Molecular Weight | 436.88 |
| Formula | C22H25ClO7 |
| CAS Number | 1210344-57-2 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related SGLT Products |
|---|
| Dapagliflozin
Dapagliflozin (BMS-512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2). |
| Canagliflozin
Canagliflozin is a potent, selective sodium glucose co-transporter 2 inhibitor. |
| Empagliflozin
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. |
| Phloridzin
Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
| Phloretin
Phloretin (NSC 407292; RJC 02792) is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). |
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