[D-Lys3]- GHRP- 6 CAS NO.136054-22-3

[D-Lys3]-GHRP-6 is a potent synthetic hexapeptide growth hormone secretagogue (GHS) and a specific, competitive antagonist of the ghrelin receptor (GHSR-1a). With the sequence His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH₂, this analog features a D-Lysine substitution at position 3, which enhances its metabolic stability and binding affinity. It acts by blocking the effects of endogenous ghrelin and synthetic agonists like GHRP-6. Supplied as a high-purity (>98%) lyophilized powder, it is a critical pharmacological tool for studying growth hormone regulation, appetite control, and GHSR-1a-mediated pathways.

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TECHNICAL SPECIFICATIONS

Item	Specification
Product Name	[D-Lys³]-GHRP-6
CAS NO.	136054-22-3
Appearance	White to off-white lyophilized powder/solid
Molecular Formula	C49H63N13O6
Molecular Weight	930.13g/mol
Purity (RP-HPLC)	≥98%
Solubility	Soluble in water, DMSO, and dilute acetic acid; readily dissolves in physiological buffers
Endotoxin	≤1.0 EU/mg
Biological Activity	Potently stimulates growth hormone (GH) secretion via binding to the ghrelin receptor (GHS-R1a).
Storage Conditions	Store at -20°C to -80°C in a sealed container, protected from moisture and light.
Stock Location	Stock in USA
MOQ	1g

1.MECHANISM OF ACTION

[D-Lys3]-GHRP-6 functions primarily as a selective and competitive antagonist at the Growth Hormone Secretagogue Receptor 1a (GHSR-1a). It binds with high affinity to the ghrelin receptor but does not activate the downstream Gq/11-protein signaling cascade. By occupying the receptor's binding site, it prevents endogenous ghrelin and other agonists (e.g., GHRP-6, GHRP-2) from binding and initiating their biological effects.

2.PRODUCT INDICATIONS

Receptor Pharmacology: Used as a selective tool to block GHSR-1a in in vitroand in vivostudies, confirming the specific involvement of this receptor in observed physiological responses.

Appetite & Metabolism Research: Investigating the role of the ghrelin system in feeding behavior, energy homeostasis, and obesity by antagonizing central GHSR-1a signaling in animal models.

Growth Hormone Axis Studies: Studying the contribution of ghrelin-mediated vs. GHRH-mediated pathways in the pulsatile secretion of GH.

Cancer Research: Exploring the role of GHSR-1a signaling in the proliferation of certain cancer cell lines (e.g., breast, prostate) where ghrelin may act as a mitogen.

Control Experiments: Serving as an essential negative control in experiments using GHSR-1a agonists to verify that observed effects are receptor-specific.

Drug Discovery: Screening and characterizing new GHSR-1a ligands by using it as a reference antagonist in competition binding assays.

3.CLINICAL EFFICACY OF PRODUCT

Preclinical Research Efficacy: It is widely recognized as a potent and selective GHSR-1a antagonist in animal and cellular models. Studies demonstrate its effectiveness in suppressing ghrelin-induced GH release and food intake.

Therapeutic Target Validation: Research using this antagonist has been instrumental in validating GHSR-1a as a therapeutic target for conditions like obesity, cachexia, and certain cancers. It helps establish cause-and-effect relationships for ghrelin's actions.

Clinical Translation Gap: This specific peptide is not a drug candidate. However, the knowledge gained from its use supports the development of small-molecule GHSR-1a antagonists currently under investigation in clinical trials for obesity and metabolic disorders.

Status: No human clinical trials have been conducted with [D-Lys3]-GHRP-6. Its value is entirely in generating robust preclinical data to guide future therapeutic development.

4.DELIVERY & SHIPPING

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