Endomorphin-1 CAS NO.189388-22-5

Endomorphin-1 (Tyr-Pro-Trp-Phe-NH₂) is a highly selective and potent endogenous μ-opioid receptor (MOR) agonist. It is a tetrapeptide that naturally occurs in the central nervous system and is known for its significant analgesic effects, often surpassing the activity of other synthetic opioids like morphine in certain contexts. This compound is widely used in neuropharmacological research to study pain pathways, receptor interactions, and potential therapeutic applications for pain management.

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TECHNICAL SPECIFICATIONS

Item	Specification
Product Name	Endomorphin-1 (Em-1)
CAS NO.	189388-22-5
Appearance	White to off-white lyophilized powder
Molecular Formula	C₃₄H₃₈N₆O₅
Molecular Weight	610.71 g/mol
Purity (RP-HPLC)	≥98%
Solubility	Soluble in sterile water (≥1 mg/mL, clear solution); soluble in DMSO (>30 mg/mL); soluble in aqueous buffers (PBS, Tris-HCl)
Endotoxin	< 1.0 EU/mg (Typical for research-grade peptides)
Biological Activity	Highly potent and selective agonist for the μ-opioid receptor (MOR). Exhibits high affinity (Ki < 1 nM) and selectivity over δ- and κ-opioid receptors. Acts as an endogenous analgesic, modulating pain perception, neurotransmitter release, and neuronal excitability in the central nervous system.
Storage Conditions	Lyophilized powder: Store at -20°C (desiccated) for 12–24 months. Reconstituted solution: Aliquot and store at -20°C; avoid repeated freeze-thaw cycles (stable for ≥1 month).
Stock Location	Stock in USA
MOQ	1g

1.MECHANISM OF ACTION

Endomorphin-1 exerts its effects by binding with high affinity and selectivity to μ-opioid receptors (MOR) in the central nervous system. Its mechanism involves:

Receptor Activation: It acts as a full agonist at the μ-opioid receptor, leading to the activation of G-proteins.
Signal Transduction: Upon binding, it inhibits adenylate cyclase activity, reducing intracellular cAMP levels.
Ion Channel Modulation: It activates G-protein-coupled inwardly rectifying potassium (GIRK) channels, leading to hyperpolarization of neurons and inhibition of calcium channels, which reduces neurotransmitter release and pain signal transmission.

2.PRODUCT INDICATIONS

This product is indicated for scientific research applications, including:

Pain Research: Investigation of analgesic mechanisms and the development of new pain therapies.
Receptor Studies: Characterization of μ-opioid receptor function and selectivity.
Neuropharmacology: Study of opioid signaling pathways and the physiological roles of endogenous opioids.
Drug Development: Screening for novel analgesics with reduced side-effect profiles.

3.CLINICAL EFFICACY OF PRODUCT

While Endomorphin-1 is not currently approved for direct clinical use in humans, its preclinical profile is promising. Research indicates that it produces potent analgesia in animal models. Notably, studies suggest that at equianalgesic doses, it may cause less severe respiratory depression compared to traditional μ-agonists like morphine, indicating a potentially improved safety profile. Its high selectivity for μ-receptors also minimizes off-target effects associated with δ- and κ-opioid receptors, making it a valuable prototype for developing safer analgesic drugs.

4.DELIVERY & SHIPPING

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Professional and Secure Packaging
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Shipping Methods
Main Method: International Air Freight

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