GLP1-R KD EndoC-βH5®
Receptor-specific activity & full signaling inactivation
KEY ADVANTAGES
Overcome GLP-1R based CHO/HEK limitations using a physiology driven model
GIPR/GCGR NATIVE EXPRESSION
PHYSIOLOGICAL RECEPTOR DISTRIBUTION
INSULIN SECRETION
BIASED-STRATEGIES RELEVANT
HTS COMPATIBLE
Future of Obesity & Type-2 Diabetes Treatments
Screening campaigns frequently generate false positive and false negative compounds, a challenge that is particularly pronounced for GIP, GLP-1, and glucagon receptors, whose physiological surface expression in native cells is inherently very limited. Moreover, cAMP and β-arrestin signaling pathways, fully coupled to insulin secretion, are critical determinants of biased GLP-1/GIP therapeutic strategies and therefore require experimental models that preserve intact, physiology-relevant signaling.
The EndoC-βH5® GLP-1R KD model is a unique, physiologically relevant human β-cell platform specifically designed to overcome these limitations. It supports screening campaigns aimed at assessing GLP-1R specificity, defining efficacy ratios of GIPR/GCGR multi-agonist candidates, and generating robust evidence for biased agonism strategies
GLP-1R specificity
GIPR/GCGR multi-agonist candidates efficacy ratio
Clinically-relevant screening
Decrease attrition compounds rate (false-positive/negative)
β-arrestin & cAMP activity access
APPLICATIONS
FUNCTIONAL VALIDATION
qPCR
Loss of GLP-1R expression
Stable invalidation
High well-to-well reproducibility
No response to GLP-1R agonist dose-reponse
Complete loss of GLP-1R function
Physiological glucose-induced function preserved
GLP-1R Agonist Insulin Secretion Dose-Response
