2134602-45-0

Product Details:

CasNo： 2134602-45-0

Molecular Formula： C19H18Cl3N3O

Appearance： White to faintly beige powder

Delivery Time： 2 weeks after order

Throughput： 1000KG/Month

Purity： 99%

SR17018 is a non-peptide, small-molecule G protein-biased agonist of the μ-opioid receptor (MOR). It preferentially activates G protein signaling (mediating analgesia) while minimizing β-arrestin2 recruitment (linked to adverse effects like respiratory depression and tolerance), making it a valuable tool for safer pain management research. Below is a comprehensive product overview.

1. Mechanism of Action

SR17018 binds to MOR (a GPCR) and stabilizes a conformation favoring coupling to inhibitory G proteins (Gαi/o). This triggers:

• Dissociation of Gαi/o-GTP and Gβγ subunits; Gαi/o inhibits adenylyl cyclase, reducing cAMP and hyperpolarizing neurons to suppress pain signaling.
• Minimal β-arrestin2 recruitment, avoiding receptor desensitization, internalization, and adverse effects associated with conventional opioids.
• Unique MOR phosphorylation dynamics (persistent vs. transient with full agonists like DAMGO), which may reverse morphine tolerance and prevent withdrawalPMC.

2. Key Applications

1. Pain Research: Development of safer analgesics with reduced respiratory depression, constipation, and tolerance risk.
2. Opioid Pharmacology: Studying MOR signaling bias, receptor phosphorylation, and biased agonist designPMC.
3. Addiction Research: Investigating reversal of morphine tolerance and prevention of opioid withdrawalPMC.
4. Neuroscience: Probing GPCR signaling in pain pathways and neuronal function.
5. Drug Discovery: Lead compound for novel MOR-targeted therapeutics with improved safety profiles.

3. Safety & Handling

• Hazard Statements: May cause skin/eye irritation; harmful if swallowed or inhaled; potential for central nervous system (CNS) depression.
• Precautionary Measures: Use in a fume hood with PPE (gloves, goggles, lab coat). Avoid contact with strong oxidizers.
• Disposal: Dispose as hazardous waste per local regulations.
• Note: For research use only; not for human or veterinary clinical applications.

4. Packaging & Quality Control

• Packaging: 10 mg, 50 mg, 100 mg, 1 g in amber glass vials (light protection).
• Quality Assurance: Each batch tested for HPLC purity, activity, solubility, and stability; COA provided.