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Brief Information

Name:Leucine-rich repeat-containing G-protein coupled receptor 5
Target Synonym:FEX,G Protein-Coupled Receptor 49,GRP49,HG38,G-protein coupled receptor HG38,GPR49,GPR67,G-protein coupled receptor 49,Leucine-rich repeat-containing G-protein coupled receptor 5,LGR5,Leucine Rich Repeat Containing G Protein-Coupled Receptor 5,G-Protein Coupled Receptor 67,Orphan G Protein-Coupled Receptor HG38
Number of Launched Drugs:0
Number of Drugs in Clinical Trials:2
Lastest Research Phase:Phase 2 Clinical

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Cat. No. Species Product Description Structure Purity Feature
LG5-C52H7 Cynomolgus Cynomolgus LGR5 / GPR49 protein, His Tag
LG5-H52H3 Human Human LGR5 / GPR49 protein, His Tag
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Part of Bioactivity data


Human R-Spondin 3 (22-146), His Tag (Cat. No. RS6-H5222) with immobilized on CM5 Chip can bind Human LGR5, His Tag (Cat. No. LG5-H52H3) with an affinity constant of 18.6 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).


Immobilized Human R-Spondin 3 Protein, Fc Tag (Cat. No. RS3-H5253) at 5 μg/mL (100 μL/well) can bind Human LGR5, His Tag (Cat. No. LG5-H52H3) with a linear range of 10-78 ng/mL (QC tested).

Synonym Name

LGR5, GPR49, GPR67, G-protein coupled receptor 49, G-protein coupled receptor 67, G-protein coupled receptor HG38, Leucine-rich repeat-containing G-protein coupled receptor 5


LGR5 (also known as GPR49) is a seven-transmembrane protein of the class A Rhodopsin-like family of GPCRs. LGR5 and LGR4 bind the R-spondins with high affinity and mediate the potentiation of Wnt/β-catenin signaling by enhancing Wnt-induced LRP6 phosphorylation. The LGR5/RSPO complex could promote Wnt signalling via the neutralization of two transmembrane E3 ligases, RNF43 and ZNRF3.

Clinical and Translational Updates

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
CNA-3103 CNA-3103 Phase 2 Clinical Carina Biotech Pty Ltd Colorectal Neoplasms Details
Petosemtamab MCLA-158 Phase 2 Clinical Merus Nv Esophageal Neoplasms; Squamous Cell Carcinoma of Head and Neck; Stomach Neoplasms; Neoplasms; Colorectal Neoplasms; Carcinoma, Non-Small-Cell Lung Details

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