CJC-1295 GHRH-R Research: Growth Hormone Axis Regulation Studies
In Vitro Research Overview
CJC-1295 is a research compound studied in cell-based assay formats for its GHRH-R (class B GPCR) Gs/cAMP/PKA signalling with DAC albumin-binding modification. Published in vitro research characterises its molecular interactions, binding affinity profiles, and downstream pathway engagement in defined cell model systems under controlled laboratory conditions. The compound represents a modified analogue of growth hormone-releasing hormone (GHRH) engineered for extended stability and receptor interaction studies.
Research applications focus on understanding pituitary somatotroph cell responses, receptor binding kinetics, and intracellular signalling cascade activation. Laboratory investigations utilise established cell lines including CHO cells transfected with human GHRH receptors, primary pituitary cell cultures, and immortalised somatotroph models for pharmacological characterisation.
Receptor Pharmacology and Mechanism of Action
GHRH Receptor Binding Characteristics
CJC-1295 acts via GHRH-R (class B GPCR) Gs/cAMP/PKA signalling with DAC albumin-binding modification. Competitive radioligand binding assays demonstrate nanomolar affinity for the GHRH receptor, with binding constants typically ranging from 0.5-2.0 nM in transfected cell systems. The compound exhibits selectivity for GHRH receptors over other related class B GPCRs including VIP, PACAP, and glucagon receptors.
Saturation binding experiments reveal specific, high-affinity interaction with GHRH receptor sites. Scatchard analysis indicates single-site binding kinetics with Hill coefficients approximating unity, suggesting non-cooperative binding behaviour. Competition studies using native GHRH(1-29) confirm receptor specificity and demonstrate comparable binding affinity profiles.
Signal Transduction Pathways
Upon receptor binding, CJC-1295 activates Gs protein-coupled adenylyl cyclase pathways, resulting in elevated intracellular cyclic adenosine monophosphate (cAMP) concentrations. Real-time cAMP accumulation assays show dose-dependent responses with EC50 values typically in the 0.1-1.0 nM range in responsive cell models.
Protein kinase A (PKA) activation follows cAMP elevation, as demonstrated through phosphorylation of downstream substrates including CREB (cAMP response element-binding protein). Western blot analysis reveals time-dependent CREB phosphorylation at Ser133 residues, indicating functional coupling to transcriptional regulatory mechanisms.
Albumin Binding Modifications
DAC Conjugation Effects
The drug affinity complex (DAC) modification involves lysine conjugation that facilitates albumin binding, extending compound stability in cell culture systems. Surface plasmon resonance studies demonstrate high-affinity albumin interaction with dissociation constants in the micromolar range. This modification does not significantly impair GHRH receptor binding affinity based on competitive binding analyses.
Albumin-bound fraction studies using equilibrium dialysis techniques show extensive protein binding (>95%) in serum-containing culture media. Despite high albumin affinity, receptor activation remains robust, suggesting effective dissociation kinetics allow productive receptor engagement.
Cell Model Applications
Somatotroph Cell Systems
Primary rat anterior pituitary cell cultures serve as physiologically relevant models for CJC-1295 receptor pharmacology studies. These heterogeneous cultures contain native somatotroph populations expressing endogenous GHRH receptors. Flow cytometry analysis confirms somatotroph identity through growth hormone immunostaining.
Immortalised GH3 and GH4C1 cell lines provide reproducible experimental platforms for mechanistic studies. These rat pituitary-derived cells maintain GHRH receptor expression and cAMP responsiveness, enabling standardised assay protocols for compound evaluation.
Transfected Cell Models
CHO-K1 cells stably transfected with human GHRH receptor cDNA offer homogeneous receptor expression for detailed pharmacological characterisation. Receptor density quantification through radioligand saturation binding typically yields 50,000-200,000 binding sites per cell, providing robust assay sensitivity.
HEK293 transient transfection systems allow rapid screening of receptor variants and mutants to probe structure-activity relationships. Luciferase reporter constructs driven by cAMP response elements enable high-throughput functional assessment of signalling pathway activation.
Research Summary
CJC-1295 represents a valuable research tool for investigating GHRH receptor pharmacology and growth hormone regulatory mechanisms in vitro. The compound demonstrates high-affinity, selective GHRH receptor binding with potent activation of Gs/cAMP/PKA signalling cascades. DAC albumin-binding modifications extend compound stability without compromising receptor interaction. Established cell models including primary pituitary cultures, immortalised cell lines, and transfected systems provide complementary platforms for comprehensive pharmacological characterisation. These in vitro systems enable detailed investigation of receptor binding kinetics, signal transduction mechanisms, and downstream cellular responses relevant to growth hormone axis regulation.
All content is intended for in vitro laboratory research purposes only. Not for human or animal consumption. Not intended to diagnose, treat, cure, or prevent any condition.
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Sarms
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Research Liquids
Albuterol 5MG/ML | 30ML with dropper
Anastrozole 1.5MG/ML | 30ML with dropper
Clomiphene 50MG/ML | 30ML with dropper
Finasteride 5MG/ML | 30ML with dropper
Letrozole 3.5 MG/ML | 30ML with dropper
LiquiCia 30MG/ML | 30ML with dropper
LiquiCia T50 50MG/ML | 30ML with dropper
LiquiClen 200MCG/ML | 30ML with dropper
Liquistane / Exemestane 25MG/ML | 30ML with dropper
LiquiTamo 20MG/ML | 30ML with dropper
LiquiVia 25MG/ML | 30 ML with dropper
T3 LIOTHYRONINE 200MCG/ML | 30ML with dropper
Toremifene Citrate 60MG/ML | 30ML with dropper
Yohimbine HCL 10MG/ML | 30ML with dropper
Research Peptides
Aicar 50MG
BPC-157 + TB-500 Blend 2mg ea/ 4MG
BPC-157 5MG
CJC-1295 + DAC 2MG
CJC-1295 | No DAC 2MG
Epithalon 10MG
Frag Premium 176-191 5MG
GHK-CU Copper Peptide 50MG
GHRP-2 5MG
GHRP-6 5MG
Hexarelin 5MG
IGF-1 DES 1MG
IGF-1 LR3 1MG
Ipamorelin 5MG
Melanotan 2 10MG
NAD+ 500MG
PT-141 / Bremelanotide 10MG
GLP-1/GIP/GCG (RT)
Selank 5MG
GLP1 (SM)
Sermorelin 5MG
TB-500 5MG
GIP/GLP-1 (TZ)
PDE5 Inhibitors
GLP-1
Diluents
Bacteriostatic Water 10ML