3081614-92-5
Chemical Structure
TGR5 agonist 10
- CAS No.: 3081614-92-5
- Formula:C25H40O6
- Molecular Weight:436.58
InChIKey: YZZPODYQSVEXEL-DFAIRORGSA-N
SMILES: O=C(O)CC[C@@H](C)[C@H]1CC[C@@]([C@]1(C)O2)([H])[C@]3([H])[C@H](OC)C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC2=O
Biological Activity: TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes[1].
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TGR5 agonist 10 | TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes. | |||||||||||||||||||||
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Keywords
