2. GPCR/G Protein
  3. G protein-coupled Bile Acid Receptor 1
  4. 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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TGR5 agonist 10

TGR5 agonist 10 Chemical Structure

CAS No. : 3081614-92-5

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TGR5 agonist 10 Related Antibodies

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Description

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].

IC50 & Target[1]

Human TGR5

0.8 μM (EC50)

Mouse TGR5

0.6 μM (EC50)

In Vitro

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.

TGR5 agonist 10 Related Antibodies
In Vivo

TGR5 agonist 10 (compound A1) (100 mg/kg; p.o.) exhibits significant glucose-lowering effects in the OGTT model in ICR mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR (8-week-old, wild-type) receiving 3 g/kg oral glucose[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose (30 minutes before glucose challenge)
Result: Showed significant glucose-lowering effects in the oral glucose tolerance test (OGTT), with comparable efficacy to positive control metformin.
Molecular Weight

436.58

Formula

C25H40O6
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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TGR5 agonist 10 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGR5 agonist 103081614-92-5G protein-coupled Bile Acid Receptor 1G-protein coupled receptor 19GPCR19TGR5GPBAR1HEK293T cellsICR miceβ-arrestin2farnesoid X receptordiabetesmTGR5cAMPlithocholic acidFXRhTGR5Inhibitorinhibitorinhibit

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