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Product Details:

CasNo： /

Molecular Formula： C₂₆H₃₀N₄O₃

Appearance： White to off-white Powder

Packing： Aluminium bag

Throughput： 300KG/Month

Purity： 99%

FH210 is an optimized G protein-biased μ-opioid receptor (μOR) agonist, structurally evolved from PZM21 via structure-based rational design. As a naphthyl-substituted acrylamide analogue, FH210 retains the PZM21-like binding mode while showing stronger Gᵢ bias and improved lipophilicity (log P = 3.9) for better CNS penetrationWiley Onli....

Compared with the parent compound PZM21, FH210 exhibits substantially attenuated β‑arrestin‑2 recruitment, with both lower potency and efficacy toward arrestin signaling. It maintains potent G protein activation and favorable μOR selectivity over δOR, κOR and other off-target GPCRs. The high-resolution cryo‑EM structure of FH210‑μOR‑Gᵢ complex reveals enhanced van der Waals contacts within the extracellular lipophilic vestibule, which stabilizes the receptor conformation disfavoring β‑arrestin couplingWiley Onli....

FH210 serves as a valuable pharmacological tool for biased μOR signaling research and a key lead compound for discovering safer non-addictive analgesics.

Key Features

• Next‑generation Gᵢ-biased μOR agonist, derived from PZM21 scaffold
• Markedly reduced β‑arrestin‑2 recruitment versus PZM21
• Higher lipophilicity, favorable for central nervous system exposure
• High-resolution cryo-EM complex structure available (PDB: 7SCG)
• Reference ligand for studying μOR extracellular vestibule biased agonism

Product Specifications

• Chemical Name: (2E)-N-[2-[[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]amino]-2-oxoethyl]-3-(naphthalen-1-yl)prop-2-enamide
• Molecular Formula: C₂₆H₃₀N₄O₃
• Molecular Weight: 446.54
• Purity: ≥99% (HPLC)
• Appearance: White to off-white solid
• Solubility: Soluble in DMSO, DMF
• Storage: Store at -20°C, protected from light and moisture
• Notice: FOR RESEARCH USE ONLY. NOT FOR HUMAN USE.

Application

• GPCR & μOR biased agonism mechanism research
• Functional assay positive control for low β‑arrestin recruitment
• Synthetic lead for novel safer analgesic candidates
• Structure‑activity relationship (SAR) study of PZM21 series

Disclaimer

This product is for laboratory research purposes only. It shall not be used for clinical, diagnostic or therapeutic applications.