Compound 7P (2-[(2-methoxyphenyl)[(4-methylphenyl)sulfonyl]amino]-N-(4-methoxy-3-pyridinyl)acetamide) is a synthetic sulfonamidoacetamide identified through a phenotypic cell-based screen of chemical libraries aimed at discovering promoters of neurite outgrowth.
Background
The compound was developed during SAR optimization of a series of dual-acting thromboxane receptor antagonist/synthase inhibitors. Compound 7P shows marked selectivity for prostaglandin I₂ synthase (PTGIS / CYP8A1) over thromboxane synthase (CYP5A1). Phenotypic screening revealed its neuritogenic activity, prompting further investigation of its neuroprotective and axon regeneration properties.
In Vitro Data
Compound 7P stimulates neurite outgrowth in primary rat (E18) neurons from the hippocampus, cerebral cortex, and retina. SAR studies showed that replacing the ethoxy-phenyl group of parent compound 1 with 4-methoxypyridine (yielding Compound 7P) improved neuritogenic activity. The effective concentration range of compound 1 was 10–20 μM; further optimization enhanced potency and metabolic stability.
In Vivo Data
In a rat model of optic nerve injury, Compound 7P induced growth of GAP-43-positive axons — a marker of neuronal process regeneration — confirming that in vitro neurite outgrowth activity translates into genuine axon regeneration in vivo. GAP-43 (growth-associated protein 43) is a well-established marker of axonal growth in the CNS.
Additional Effects
In vitro studies on HeLa cells demonstrated pro-apoptotic activity: Compound 7P increased the proportion of cells in G0/G1 and S phases, decreased G2/M fraction, and modulated expression of C-caspase-3, C-caspase-9, Bcl-2, and Bax — suggesting potential utility in oncology target research.
Physicochemical Properties
Molecular weight: 441.5 g/mol. Appearance: white to off-white powder. Soluble in organic solvents (DMSO, DMF); poorly soluble in water.
Storage
Room temperature (+15°C…+25°C), airtight container, protected from light and moisture. Shelf life ≥24 months under proper conditions.
BIOLABCHEMICALS