| Hazard Information | Back Directory | [Description]
RO5527239 is a potent, orally available GPBAR1 agonist. | [Uses]
RO5527239 is an orally active TGR5 agonist, that induces a stimulatory response from intestinal L cells and specificially secrets the endogenous hormone GLP-2[1]. | [in vivo]
RO5527239 (30 mg/kg, p.o. for 10 days) stimulates the TGR5 receptor, upregulates L cells and L cells hormone GLP-2, triggers a GLP-2-dependent intestinal adaption in C57BL/6N mice[1]. | Animal Model: | GLP-2r-/- and GLP-2r+/+ C57Bl/6N mice[1] | | Dosage: | 30 mg/kg | | Administration: | p.o. for 10 days | | 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. |
| [References]
[1] Hunt JE, et al., Pharmacological activation of TGR5 promotes intestinal growth via a GLP-2-dependent pathway in mice. Am J Physiol Gastrointest Liver Physiol. 2020 May 1;318(5):G980-G987. DOI:10.1152/ajpgi.00062.2020 |
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