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Cat. No. Product Name Information
PC-20559

(R)-YNT-3708

OX1R agonist

(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).
PC-49188

OBPt-9

OXR1/2 potentiator

OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A.
PC-38360

Firazorexton

OX2R agonist

Firazorexton (TAK-994) is a potent, selective, orally available and brain-penetrant agonist of orexin 2 receptor (OX2R) with EC50 of 19 nM against recombinant human OX2R, 700-fold selectivity against OX1R.
PC-73244

YNT-185

OX2R agonist

YNT-185 is a potent, selective orexin type-2 receptor (OX2R) agonist with EC50 of 28 nM, 100-fold selectivity over OX1R.
PC-72749

TAK-925

OX2R agonist

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).
PC-60727

ACT-541468

Orexin receptor antagonist

ACT-541468 (Nemorexant) is a potent, selective, dual orexin receptor 1 and 2 (OX1 and OX2) antagonist with Kb of 0.52 and 0.78 nM, respectively.
PC-60062

Suvorexant

Orexin receptor antagonist

Suvorexant (MK-4305, MK4305) is a potent, CNS penetrant, orally available, dual orexin receptor antagonist with Ki of 0.55 and 0.35 nM for OX1R and OX2R, respectively.
PC-42731

SB-334867 free base

OX1R inhibitor

SB-334867 is the first selective Orexin-1 receptor (OX1R) antagonist with pKb of 7.4, displays 50-fold selectivity over OX2R (pKb 5.7).
PC-42733

TCS 1102

Orexin receptor inhibitor

TCS 1102 is a potent and selective dual Orexin receptor antagonist with Ki of 0.2/3 nM for hOX2R/hOX1R respectively.
PC-21917

JNJ-61393215

OX1R inhibitor

JNJ-61393215 (Tebideutorexant) is a potent, selective orexin-1 receptor (OX1R) antagonist with pKi values of 8.17 and 8.13 for human OX1R and rat OX1R, respectively.
PC-21740

CVN766

OX1R inhibitor

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.
PC-21731

CVN45502

OX1R inhibitor

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).

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