Name | [(3S)-6-({2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy]-3-biphenylyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid |
Synonyms | CS-54 TAK875 TAK875 TAK-875 TAK 875. TAK-875,TAK875 TAK-875(Fasiglifam) (3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid [(3S)-6-({2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy]-3-biphenylyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid 3-Benzofuranacetic acid, 6-[[2',6'-diMethyl-4'-[3-(Methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]Methoxy]-2,3-dihydro-, (3S)- 3-Benzofuranacetic acid, 6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-, (3S)- |
CAS | 1000413-72-8 |
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. |