| Molecular Formula | C29H32O7S |
| Molar Mass | 524.63 |
| Density | 1.252 |
| Melting Point | 123-127°C |
| Boling Point | 739.1±60.0 °C(Predicted) |
| Solubility | Acetonitrile (Slightly), DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 4.36±0.10(Predicted) |
| Storage Condition | Refrigerator |
| introduction | Fasiglifam (TAK-875) is a selective GPR40 agonist. EC50 is 14 nM in CHO cell line expressing human GPR40, which is 400 times more effective than oleic acid. TAK-875 exhibited potent agonist activity and high binding affinity for human GPR40 receptors with a Ki of 38 nM. The TAK-875 showed a weak affinity for the rat GPR40 receptor with a Ki of 140 nM. TAK-875 showed good selectivity, with little agonistic effect on other members of the FFA receptor family, EC50 >10 μM. |
| application | the latest research shows that TAK-875 is a new drug for the treatment of type 2 diabetes. its effect on improving blood sugar control is similar to glimepiride, but the risk of hypoglycemia is significantly lower than the latter. It is a new oral drug that enhances insulin secretion in a glucose-dependent manner. That is, when the blood sugar level is normal, TAK-875 has no effect on insulin secretion. Therefore, TAK-875 can not only effectively control the rise of blood sugar, but also minimize the risk of hypoglycemia. |