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Cat. No.: HY-116453

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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.

For research use only. We do not sell to patients.

CAS No.: 1354812-99-9
Formula: C₂₈H₃₁N₃O₃
Molecular Weight:457.56

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

RO5527239 Chemical Structure

CAS No.: 1354812-99-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.004 μM Compound: (R)-29, RO5527239	Agonist activity at recombinant human GPBAR1 expressed in CHO cells Agonist activity at recombinant human GPBAR1 expressed in CHO cells	[PMID: 23831134]
CHO	EC₅₀	0.028 μM Compound: (R)-29, RO5527239	Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells Agonist activity at recombinant mouse GPBAR1 expressed in CHO cells	[PMID: 23831134]
NCI-H716	EC₅₀	0.08 μM Compound: (R)-29, RO5527239	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	[PMID: 23831134]

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].

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

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.

Chemical Information

CAS No. 1354812-99-9
Molecular Weight 457.56
Formula C₂₈H₃₁N₃O₃
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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