| DC11439 |
Nemorexant
Featured
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ACT-541468 is a dual orexin receptor antagonist. |
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| DC7692 |
Almorexant HCl (Act-078573)
Featured
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Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. |
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| DC8173 |
Lemborexant(E2006)
Featured
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Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia. |
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| DC9297 |
MDK-5220(Orexin-2 receptor agonist)
Featured
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MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%) |
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| DC9966 |
MK-1064
Featured
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MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia. |
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| DC7646 |
MK3697 |
MK-3697 is a third insomnia drug, currently being developed by Merck. MK-3697 is a potent and selective Orexin receptor antagonist with Ki = 0.95 nM. |
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| DC7495 |
SB-334867 HCl
Featured
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SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. |
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| DC8419 |
SB-334867
Featured
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SB-334867 is a selective orexin-1 (OX1) receptor antagonist. |
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| DC7277 |
SB-408124
Featured
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SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. |
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| DC9573 |
SB-674042
Featured
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SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.
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| DC5017 |
Suvorexant
Featured
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Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.Suvorexant is an analytical reference standard categorized as a diazepane sedative.Formulations containing suvorexant show abuse potential similar to zolpidem in recreational polydrug users with a history of sedative and psychedelic drug use.2 Suvorexant is regulated as a Schedule IV compound in the United States. This product is intended for use in analytical forensic applications. |
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| DC7513 |
TCS 1102
Featured
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TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). |
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| DC11461 |
TCS-OX2-29
Featured
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TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1. |
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| DC28246 |
EMPA
Featured
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EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively. |
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| DC28252 |
Seltorexant hydrochloride |
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain. |
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| DC41022 |
Orexin receptor antagonist 3 |
Orexin receptor antagonist 3 (example 216) is an orexin receptor antagonist, which is extracted from the patent WO2011050198A1. |
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| DC41789 |
[Ala11,D-Leu15]-Orexin B(human) |
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM). |
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| DC41790 |
[Ala11,D-Leu15]-Orexin B(human) TFA |
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM). |
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| DC41791 |
OXA(17-33) |
OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ～23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM). |
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| DC41792 |
OXA(17-33) TFA |
OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ～23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM). |
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| DC42501 |
Orexin receptor antagonist 2 |
Orexin receptor antagonist 2 (compound 30) is a potent orexin receptor antagonist with pKis of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia. |
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| DC45872 |
YNT-185 dihydrochloride |
YNT-185 dihydrochloride 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 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models. |
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| DC45873 |
JNJ-54717793 |
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. |
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| DC46039 |
YNT-185 |
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. |
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| DC48420 |
Orexin B, rat, mouse TFA |
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. |
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| DC50258 |
TCS-OX2-29 hydrochloride |
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. |
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| DC70412 |
Firazorexton |
Firazorexton is a potent, selective, experimental orexin 2 receptor (OX2R) agonist. |
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| DC70676 |
OX2R agonist 1 |
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. |
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| DC70823 |
TAK-925
Featured
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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. |
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| DC70884 |
Vornorexant |
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. |
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