RO5527239
RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2.
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- CAS No.: 1354812-99-9
- Formule: C28H31N3O3
- Masse moléculaire:457.56
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.004 μM
Compound: (R)-29, RO5527239
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Agonist activity at recombinant human GPBAR1 expressed in CHO cells
Agonist activity at recombinant human GPBAR1 expressed in CHO cells
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[PMID: 23831134] |
| CHO | EC50 |
0.028 μM
Compound: (R)-29, RO5527239
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Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells
Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells
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[PMID: 23831134] |
| NCI-H716 | EC50 |
0.08 μM
Compound: (R)-29, RO5527239
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Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
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[PMID: 23831134] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GLP-2r-/- and GLP-2r+/+ C57Bl/6N mice[1]
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Dosage:30 mg/kg
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Administration:p.o. for 10 days
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Result:Increased GLP-1 and GLP-2 concentrations in the colon, gallbladder weight with both genotype. Increased villus height in the duodenum and decreased colon length in GLP-2r+/+ mice.
Chemical Information
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CAS No. 1354812-99-9
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Masse moléculaire 457.56
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Formule C28H31N3O3
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SMILES
O=C(C1CCN(C2=CC=C([C@H](C3=CC=CC=C3C)C/C(C4=CC(C)=NC=C4)=N\O)C=C2)CC1)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.
Protocole
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RO5527239 Related Classifications
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