Home > Inhibitors & Agonists > GPCR > Orexin Receptor
Cat. No. Product name CAS No.
DC11439 Nemorexant

ACT-541468 is a dual orexin receptor antagonist.

1505484-82-1
DC7692 Almorexant HCl (Act-078573) Featured

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.

913358-93-7
DC8173 Lemborexant(E2006) Featured

Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.

1369764-02-2
DC9297 MDK-5220(Orexin-2 receptor agonist) Featured

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%)

1796565-52-0
DC9966 MK-1064 Featured

MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.

1207253-08-4
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.

1224846-01-8
DC7495 SB-334867 HCl

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

249889-64-3
DC8419 SB-334867

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

792173-99-0
DC7277 SB-408124

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.

288150-92-5
DC9573 SB-674042

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.

483313-22-0
DC5017 Suvorexant (MK-4305) Featured

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.

1030377-33-3
DC7513 TCS 1102 Featured

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).

916141-36-1
DC11461 TCS-OX2-29 Featured

TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.

372523-75-6
DC28246 EMPA Featured

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.

680590-49-2
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.

1293284-49-7
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