2230597-99-4
Chemical Structure
Xelaglifam
Synonym(s): IDG-16177
- CAS No.: 2230597-99-4
- Formula:C30H28FNO5
- Molecular Weight:501.55
IUPAC Name: 1-(2-((3R,5R,8R,9R,10S,13S,14S,15R,17S)-3-hydroxy-3,13,15-trimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl)-1H-pyrazole-3-carbonitrile
InChIKey: IJUWQJZOUDTENA-HRRBBWQUSA-N
SMILES: FC1=C(C(CC2)=C(C3=CN=C(O[C@@H]4CCOC4)C=C3)C=C1)[C@@H]2OC5=CC=C(C=C5)[C@@H](C#CC)CC(O)=O
Biological Activity: Xelaglifam is an orally active GPR40/FFAR1 agonist and PPARγ coactivator recruitment inhibitor (IC50 74.7 µM). Xelaglifam activates Gq/IP3/Ca2+ and β-arrestin, stimulates glucose-dependent insulin secretion from pancreatic β cells, improves glucose tolerance, reduces fasting hyperglycemia, protects pancreatic β cells, inhibits DP1, BSEP (IC50 14.3 µM), MRP2 (39.9 µM) and MRP4 (4.4 µM), activates FXR, regulates bile acid homeostasis, and modulates mitochondrial function, membrane potential and cellular ATP. Xelaglifam can be used for research on type 2 diabetes[1][2].
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Xelaglifam | Xelaglifam is an orally active GPR40/FFAR1 agonist and PPARγ coactivator recruitment inhibitor (IC50 74.7 µM). Xelaglifam activates Gq/IP3/Ca2+ and β-arrestin, stimulates glucose-dependent insulin secretion from pancreatic β cells, improves glucose tolerance, reduces fasting hyperglycemia, protects pancreatic β cells, inhibits DP1, BSEP (IC50 14.3 µM), MRP2 (39.9 µM) and MRP4 (4.4 µM), activates FXR, regulates bile acid homeostasis, and modulates mitochondrial function, membrane potential and cellular ATP. Xelaglifam can be used for research on type 2 diabetes. | |||||||||||||||||||||
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References
- [1]. Yoon J, et al. Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2024 Aug;177:117044. [Content Brief]
- [2]. Yoon J, et al. Lower hepatotoxicity risk in Xelaglifam, a novel GPR40 agonist, compared to Fasiglifam for type 2 diabetes therapy. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2024 Dec;181:117674.
