Abstract: The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds and/or compositions treat or prevent skin disorders or diseases associated with hypopigmentation in the subject. In other embodiments, the compounds and/or compositions comprise an estrogen derivative or analog that binds to the non-canonical sex steroid hormone receptor GPER and does not bind to the canonical nuclear estrogen receptor (ER).