Orexin B, human (TFA)

Human orexin B (TFA)

C123H212N44O35S.C2HF3O2

H2O

GPCR/G Protein; Neuronal Signaling

Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively. IC50 & Target: Ki: 420 nM (OX1), 36 nM (OX2)^[1]. In Vitro: Orexin B is derived by proteolytic amino acid precursor, prepro-orexin, which is encoded by a gene localized to chromosome 17q21 in humans. In radioligand binding studies, Orexin B has a higher affinity for the OX2 receptor^[1].
Human Orexin B has two amino acid substitutions when compared with the rodent sequence. OX2 receptor is indeed a high-affinity receptor for human orexin B, with an IC₅₀ of 36 nM in the binding assay and an EC₅₀ of 60 nM in the [Ca²⁺]i transient assay. Human Orexin B has significantly lower affinity for the human OX1: the calculated IC₅₀ in the competitive binding assay and the EC₅₀ in the [Ca²⁺]i transient assay are 420 nM and 2500 nM for human orexin-B, respectively^[2]. In Vivo: Human Orexin B significantly augments food intake; at the 2 hr time point, 5- and 12-fold stimulation of food consumption is observed by 3 nM and 30 nM orexin-B, respectively^[2].