Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D0M0WV
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| Former ID |
DIB002820
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| Drug Name |
Fasiglifam hemihydrate
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| Synonyms |
Fasiglifam hemihydrate; 1374598-80-7; UNII-8LDT91CH8A; 8LDT91CH8A; TAK-875 Hemihydrate; Fasiglifam hydrate (JAN); DTXSID80160191; MolPort-035-395-707; EX-A2165; s2637; AKOS025404925; 3-Benzofuranacetic acid, 6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)(1,1'-biphenyl)-3-yl)methoxy)-2,3-dihydro-, hydrate (2:1), (3S)-; (3S)-6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy) biphenyl-3-yl)methoxy)-2,3-dihydro-l-benzofuran-3-yl)acetic acid hydrate; SC-95595; BC600332; (3S)-6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy)
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| Drug Type |
Small molecular drug
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| Indication | Type-2 diabetes [ICD-11: 5A11; ICD-9: 250] | Phase 3 | [1] | |
| Company |
Apollo Scientific
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| Structure |
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Download2D MOL |
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| Formula |
C58H66O15S2
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| Canonical SMILES |
CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.O
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| InChI |
1S/2C29H32O7S.H2O/c2*1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24;/h2*4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31);1H2/t2*23-;/m11./s1
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| InChIKey |
OJXYMYYDAVXPIK-IWKNALKQSA-N
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| CAS Number |
CAS 1374598-80-7
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| PubChem Compound ID | ||||
| PubChem Substance ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Free fatty acid receptor 1 (GPR40) | Target Info | Modulator | [2], [3] |
| KEGG Pathway | Insulin secretion | |||
| Reactome | G alpha (q) signalling events | |||
| Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion | ||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | |||
| Incretin Synthesis, Secretion, and Inactivation | ||||
| Gastrin-CREB signalling pathway via PKC and MAPK | ||||
| Integration of energy metabolism | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | ClinicalTrials.gov (NCT02015780) Fasiglifam in Type 2 Diabetic Subjects With Chronic Kidney Disease Stage 4 or 5 on Hemodialysis. U.S. National Institutes of Health. | |||
| REF 2 | A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One. 2013 Oct 10;8(10):e76280. | |||
| REF 3 | TAK-875, a GPR40/FFAR1 agonist, in combination with metformin prevents progression of diabetes and beta-cell dysfunction in Zucker diabetic fatty rats. Br J Pharmacol. 2013 Oct;170(3):568-80. | |||
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