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
