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OX Receptor

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
E4740 TAK-861 (Oveporexton) Oveporexton (TAK-861) is a potent, orally bioavailable agonist of orexin receptor 2 (OX2R), with an EC50 of 2.5 nM in calcium mobilization assays. It induces dose-dependent membrane depolarization in histaminergic neurons within the mouse tuberomammillary nucleus (TMN) with an EC50 of 31.7 nM.
S2160 Almorexant HCl Almorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.
Cell Reports, June 16, 2020, 107779
bioRxiv, July 10, 2024, 2024.07.06.602357
Research Square (Preprint), December 2022, nan
Verified customer review of Almorexant HCl
S7585 SB-334867 SB-334867 is a selective orexin-1 (OX1) receptor antagonist.
Journal of Neuroinflammation, June 15, 2020, 187
Behavioural Brain Research, July 26, 2023, 114491
J Pharmacol Exp Ther, 2025, 392(7):103624
E0107 EMPA EMPA is a selective OX2 receptor antagonist and binds to human and rat OX2-HEK293 membranes with Kd values of 1.1 and 1.4 nM respectively.
Eur Heart J, 2024, 31:ehae472.
Oxid Med Cell Longev, 2022, 2022:1122494
S1545 SB408124 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.
Nat Chem Biol, 2017, 13(2):235-242
E7098 Orexin A (human, rat, mouse) Orexin A (human, rat, mouse) (hypocretin‑1) is a 33‑amino‑acid excitatory neuropeptide that orchestrates diverse central and peripheral processes by binding and activating two G protein‑coupled receptors, the orexin‑1 receptor (OX1R) and the orexin‑2 receptor (OX2R). It also plays a role in the regulation of feeding behavior and acts as an effective anti‑nociceptive and anti‑hyperalgesic agent in mice and rats.
American Journal of Physiology-Heart and Circulatory Physiology, April 01 2017, H808-H817
S6717 TCS-OX2-29 TCX-OX2-29 is a OX2R antagonist (pKi = 7.5) that exhibits >250-fold selectivity for hOX2R compared with hOX1R (IC50s = 40 nM and >10,000 nM, respectively).
J Pharmacol Exp Ther, 2025, 392(7):103624
S3503New Seltorexant Seltorexant (JNJ-42847922) is a potent and selective antagonist of the orexin-2 receptor (OX2R) exhibiting strong affinity (pKi ~8.0) for human OX2R. It promotes sleep onset and demonstrates antidepressant effects in major depressive disorder (MDD) patients with insomnia by blocking hyperarousal linked to depression and sleep disturbance.
S6726 MK1064 MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM.

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