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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- CAS No.: 3081614-92-5
- Formule: C25H40O6
- Masse moléculaire:436.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Human TGR5 0.8 μM (EC50) |
Mouse TGR5 0.6 μM (EC50) |
TGR5 agonist 10 (compound A1) has lower potency for β-arrestin2 recruitment (EC50 = 26.5 μM) than for cAMP accumulation in HEK293T cells[1].
TGR5 agonist 10 (10-20 μM; 8 h) does not activate FXR at 10 μM or 20 μM in HEK293T cells, indicating selectivity for TGR5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (8-week-old, wild-type) receiving 3 g/kg oral glucose[1]
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Dosage:100 mg/kg
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Administration:p.o.; single dose (30 minutes before glucose challenge)
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Result:Showed significant glucose-lowering effects in the oral glucose tolerance test (OGTT), with comparable efficacy to positive control metformin.
Chemical Information
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CAS No. 3081614-92-5
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Masse moléculaire 436.58
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Formule C25H40O6
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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