1-(β-D-glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienyl-methyl) benzene
canagliflozin
CAS: 842133-18-0;928672-86-0
Molecular Formula: 2(C24H25FO5S).H2O
1-(β-D-glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienyl-methyl) benzene - Names and Identifiers
1-(β-D-glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienyl-methyl) benzene - Physico-chemical Properties
| Molecular Formula | 2(C24H25FO5S).H2O |
| Molar Mass | 462.53 |
| Density | 1.4±0.1 g/cm3 |
| Melting Point | 94-96°C |
| Boling Point | 642.9±55.0 °C at 760 mmHg |
| Flash Point | 342.6±31.5 °C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
| Stability | Hygroscopic |
| MDL | MFCD18251436 |
| In vitro study | Canagliflozin inhibits Na + -dependent 14 C-AMG uptake in CHO-hSGLT2 cells, with an IC 50 of 4.4±1.2 nM. Similar IC 50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC 50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14 C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC 50 of 684±159 nM and >1,000 nM, respectively. |
| In vivo study | Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats. Animal Model: Diet-induced obese, insulin resistantmice (DIO) Mice Dosage: 30 mg/kg Administration: Oral gavage; daily; 4 weeks Result: Reduced BG levels, respiratory exchange ratio, and body weight gain. Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats Dosage: 3 mg/kg Administration: Oral gavage; daily; 3 weeks Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight. |
1-(β-D-glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienyl-methyl) benzene - Introduction
Canagliflozin inhibits Na - dependent 14C-AMG uptake in a concentration-dependent fashion. It is a novel C- glucoside with thiophene ring.
Last Update：2022-10-16 17:29:19
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