ox1

TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2 3 nM for OX2 1 receptors).

SB-674042 is a potent, selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50 values of 3.76 nM and 531 nM, respectively. SB-674042 is suitable for the treatment of depression.

SB-334867 free base (SB334867A free base) is a selective antagonist of the orexin-1 (OX1) receptor.

ALOX15-IN-2 is a potent inhibitor of ALOX15 linoleate oxygenase activity, inhibiting the oxidation of linoleic acid (LA) and arachidonic acid (AA), the immediate homologs of ALOX15, with IC50s of 1.55 and 2.79 μM, respectively.

IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.

OX1a is an orco antagonist agent which acts as a non-competitive inhibitor of odorant activation of an insect OR.

OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacteria.

ALOX15-IN-1 (compound 8b) is a selective and potent inhibitor of rabbit and human ALOX15 linoleate oxygenase activity, targeting the direct homologues of ALOX15 linoleic acid (LA) with an IC50 of 0.04 μM and arachidonic acid (AA) with an IC50 of 2.06 μM.

Potent and selective peptide orexin OX1 receptor agonist (EC50 values are 8.29 and 187 nM for OX1 and OX2 receptors respectively). Truncated form of orexin A.

SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

Orexin B, rat, mouse Acetate (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.

OXA (17-33) acetate is a more potent agonist of orexin-1 receptor (OX1, EC50 = 8.29 nM)) over OX2 (EC50 = 187 nM).

SB-408124 Hydrochloride is a non-peptide OX1 receptor antagonist(Ki of 57 nM and 27 nM in both whole cell and membrane, respectively).

Filorexant (MK-6096) is an orally bioavailable, effective, and selective reversible antagonist of OX1 and OX2 receptors, with (Ki <3 nM).

(R)-YNT-3708 is a specific Orexin 1 receptor (OX1R) agonist with an EC50 value of 7.48 nM for OX1R. The EC50 ratio of OX2R to OX1R is 22.5. This compound demonstrates analgesic and enhancing effects by activating OX1R in mice.

ACT-335827 is an orally available, brain-penetrant, orexin type 1 receptor-selective antagonist, with IC50 values of 6 nM for OXR1 and 417 nM for OXR2. It is suitable for studies related to neurological disorders [1].

Almorexant (ACT 078573) 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.

Potent and selective orexin OX2 receptor agonist (EC50 = 28 nM at human OX2 expressed in CHO cells). Displays approximately 100-fold selectivity for OX2 over OX1 (EC50 = 2.75 μM at human OX1 expressed in CHO cells). Depolarizes OX2-expressing histaminergic neurons in mouse brain slices. Increases wake time in wild type mice. Suppresses cataplexy-like symptoms in OX knockout mice. Nagahara et al (2015) Design and synthesis of non-peptide, selective orexin receptor 2 agonists. J.Med.Chem. 58 7931 PMID:26267383 |Irukayama-Tomobe et al (2017) Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc.Natl.Acad.Sci.USA. 144 5731 PMID:28507129

TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1.

IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

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.

[Ala11,D-Leu15]-Orexin B(human) TFA is a potent, selective agonist for the orexin-2 receptor (OX2), demonstrating 400-fold higher selectivity for OX2 (EC50=0.13 nM) compared to the orexin-1 receptor (OX1) with an EC50 of 52 nM.

OXA(17-33) TFA is a potent and selective agonist for the orexin-1 receptor (OX1), with approximately 23-fold higher affinity for OX1 (EC50 = 8.29 nM) compared to the orexin-2 receptor (OX2) (187 nM) [1].