The town was established as San Felipe y Santiago in 1585 by Antonio Ruiz, Bartolomé de Mondragón, Tomás de Soberanes, Juan Martínez del Castillo y Juan Caballero. By 1590, Ruiz was its alcalde mayor, and it held nine people who eked out a living, but the situation improved through their discovery of the mines of Chínipas, and the arrival of the Jesuits in 1591. At the end of the sixteenth century, Ruiz wrote his history where he detailed the early history of San Felipe y Santiago, and Sinaloa.
This was the base for Diego de Hurdaide's subjugation of the Sinaloas, Tehuecos, Ahomes and Zuaques and the extension of Spanish control over the Fuerte River valley, and thus to the northern edge of modern Sinaloa.
Sinaloa serves as the municipal seat for the surrounding municipality (municipio) of Sinaloa, Sinaloa. The municipality reported 88,282 inhabitants in the 2010 census. It is a former capital of the Mexican state of Sinaloa.