Sesamol has been studied extensively in the past two decades for its curative role in various diseases owing to its antioxidant potential. In vitro and in vivo pre-clinical studies indicate diverse role of sesamol in ailments connected by a common denominator of oxidative stress. These include antioxidant, anti-mutagenic, neuroprotective, hepatoprotective, cardioprotective, chemopreventive and anti-ageing properties. However, in depth investigation of its important characteristics including its oral pharmacokinetics is warranted, before evaluating this molecule for clinical application. The present study was undertaken to determine the physicochemical properties viz. solubility, log P, pK_a and distribution coefficient of sesamol, coupled with its regional permeability through rat GIT. Single dose oral pharmacokinetic and tissue distribution studies of sesamol were also conducted in rats. The results indicate sesamol to be a molecule with appropriate aqueous solubility (∼38.8 mg mL⁻¹) and log P (1.29); the pK_a of sesamol was found to be 9.79 and it exhibited a distribution coefficient of >1. Sesamol was well absorbed throughout the GIT and showed an oral bioavailability of 95.61%. Sesamol is widely distributed in rat tissue with the highest concentration in the kidneys followed by lungs, brain, and liver. In spite of a favorable bioprofile, the wide distribution, small t_1/2 and fast clearance of sesamol indicate a need for packaging it into a suitable delivery system.