Advance Your Melanocortin Receptor Drug Discovery with Our High-Quality GPCR Stable Cell Lines‌

GPCRs represent the largest class of drug targets, with over 35% of FDA-approved drugs targeting these receptors. Their involvement in diverse physiological pathways makes them ideal for treating complex diseases. However, developing GPCR-targeted drugs requires robust preclinical models to assess ligand binding, signaling efficacy, and toxicity.

Melanocortin receptors (MCRs) are a subfamily of G protein-coupled receptors (GPCRs) critical for regulating physiological processes such as energy homeostasis, pigmentation, inflammation, and exocrine gland function. As druggable GPCRs, they have emerged as promising targets for treating obesity, metabolic disorders, skin diseases, and rare genetic conditions. Dysregulation of melanocortin receptor (MCR) signaling is linked to multiple pathologies, making these receptors focal points for innovative drug development.

There are five known members of the melanocortin receptor system, each with differing specificities for melanocortins.

Member	Function	Disease	Application
MC1R	Regulates melanin synthesis, immune & inflammatory responses	Pigmentation disorders, Inflammatory conditions	Studying UV protection and melanocyte biology
MC2R	Adrenal cortex function and cortisol synthesis	Congenital adrenal hyperplasia	Adrenal function research, endocrine disorder studies
MC3R	Energy metabolism, appetite regulation, and immune homeostasis	Early-onset obesity	Obesity and inflammation research
MC4R	Energy balance	Severe early-onset obesity	Obesity drug screening and leptin pathway studies
MC5R	Regulates exocrine gland function and immune cell activity	Hypohidrosis, acne	Skin physiology and immunology studies

Stable cell lines expressing functional melanocortin receptors (MCRs) provide consistent, reliable platforms for high-throughput screening (HTS), mechanistic studies, and lead optimization.

1) High-Throughput Screening (HTS): Enable rapid identification of hit compounds via ligand binding assays.

2) Signaling Pathway Analysis: Monitor cAMP to assess agonist/antagonist efficacy.

3) Toxicity and Safety Testing: Evaluate off-target effects in a controlled cellular environment.

4) Pharmacodynamic Studies: Model receptor desensitization, internalization, and long-term signaling effects.

Creative Biogene owns a proprietary technology platform for GPCR stable cell line construction. Our platform has successfully developed a number of functionally validated GPCR stable cell line products which cover various type of GPCR targets including melanocortin receptors (MCRs). These stable cell lines have undergone rigorous testing to ensure high GPCR expression, robust GPCR functional activity, free of contamination etc. Our validated stable cell lines provide the consistency and physiological relevance needed to advance your pipeline.

Product List

Product Name	Cat#	Price
Human MC1R Stable Cell Line - HEK293	CSC-RG01852	Inquiry
Human MC2R Stable Cell Line - HEK293	CSC-RG01853	Inquiry
Human MC3R Stable Cell Line - HEK293	CSC-RG01854	Inquiry
Human MC4R Stable Cell Line - HEK293	CSC-RG01855	Inquiry
Human MC5R Stable Cell Line - HEK293	CSC-RG01856	Inquiry

Product Applications

1) Academic research (e.g., signal transduction).

2) Pharmaceutical drug discovery (e.g., hit identification, lead optimization).

3) Contract research organizations (CROs) for preclinical assay development.

Highlights

1) High GPCR expression levels validated by real-time qPCR.

2) Functional responsiveness to known ligands (e.g., α-MSH).

3) Ready for immediate use in binding assays (e.g., cAMP experiments).

4) Contamination-free (e.g., mycoplasma, bacterial, fungi etc.).

5) Customization options for a preferred cell background.

6) Fast turnaround‌ with full technical support.

Representative Data

1) High-level gene expression verified by QPCR

Human MC1R overexpression level in HEK293-Human-MC1R measured by qPCR.

Human MC3R overexpression level in HEK293-Human-MC3R measured by qPCR.

Human MC4R overexpression level in HEK293-Human-MC4R measured by qPCR.

Human MC5R overexpression level in HEK293-Human-MC5R measured by qPCR.

2) Robust receptor activity verified by cAMP Assay

Human MC1R function activities in HEK293-Human-MC1R measured by cAMP assay kit.

Human MC3R function activities in HEK293-Human-MC3R measured by cAMP assay kit.

Human MC4R function activities in HEK293-Human-MC4R measured by cAMP assay kit.

Human MC5R function activities in HEK293-Human-MC5R measured by cAMP assay kit.

3) Mycoplasma-free detected by PCR & MycoAlert kit

description：Mycoplasma PCR detection data of HEK293 expressing melanocortin receptors (MCRs).

MycoAlert Mycoplasma Detection Data
Luminescence	A Value	B Value	B/A ratio	Result
Negative Control	2517	593	0.23560	/
Positive Control	21213	828334	39.04841	/
HEK293-Human-MC1R	9527	5974	0.62706	Negative/-
HEK293-Human-MC3R	8768	6018	0.68636	Negative/-
HEK293-Human-MC4R	18490	10262	0.55500	Negative/-
HEK293-Human-MC5R	9438	5445	0.57692	Negative/-