JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.

YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models.

Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.

TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.

Firazorexton is a potent, selective, experimental orexin 2 receptor (OX2R) agonist.

OX2R agonist 1 is a potent, selective, small-molecule agonist of orexin receptor 2 (OX2R) with pEC50 of 8.28, >300-fold selectivity over OX1R.

TAK-925 (Danavorexton) is a potent, selective, and brain-penetrant Orexin 2 receptor (OX2R) agonist with EC50 of 5.5 nM, no significant inhibition on OX1R (IC50>100 uM).TAK-925 also showed good selectivity against 106 off-target enzymes and receptors.

Vornorexant (TS-142, ORN0829) is a potent dual orexin 1 and 2 receptor antagonist with IC50 of 1.05 and 1.27 nM for hOX1R and hOX2R, resepctively.Vornorexant (TS-142, ORN0829) exhibited potent sleep-promoting effects at a po dose of 1 mg/kg in a rat polysomnogram study.Vornorexant (TS-142, ORN0829) is a viable candidate and is currently in clinical development for the treatment of insomnia.

ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.

Nivasorexant is a potent orexin receptor antagonist.

Tebideutorexant is a potent orexin receptor antagonist. Tebideutorexant can be used for insomnia research.

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.

OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A.