RGNCY-0002 (Euodenine A Derivative)

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Euodenine A is a small molecule natural product agonist of the human TLR4 receptor (Ec50=0.39uM). It is a human-selective agonist that is CD14-independent, and it requires both TLR4 and MD-2 for full efficacy. Testing for immunomodulation in PBMC cells indicated that compounds like Euodenine A could modulate the Th2 immune response without causing lung damage.

Systematic Name: (1R,2R,2aR,10aS)-1 -cyclopentyl-2-(3,4-dimethoxyphenyl)-10,10-dimethyl-2,2a,10,10a-tetrahydro-1Hcyclobuta[4,5]pyrano[3,2-c]quinolin-3(4H)-one

SMILES: O=C1NC2=CC=CC=C2C3=C1[C@@H]4[C@H](C5=CC=C(OC)C(OC)=C5)

Molecular Weight: 459.58

Formula: C29H33NO4

Reference: Neve, Juliette E., et al. "Euodenine A: A Small-Molecule Agonist of Human TLR4." Journal
of Medicinal Chemistry
57.4 (2014): 1252-1275.

PMID: 24471857

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Tags: TLR4, RGNCY-0002, Euodenine A, CD14, immunity, Th2