Date published: 2026-4-28

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Orexin R-2 Inhibitors

Orexin R-2, a G protein-coupled receptor intricately involved in the regulation of sleep-wake cycles and various physiological processes, can be effectively modulated by a specific class of chemical inhibitors. Among these inhibitors are TCS-OX2-29, EMPA, SB-334867, Almorexant, Suvorexant, JNJ-10397049, Filorexant, Lemborexant, ACT-462206, TCS-OX2-29 dihydrochloride, Filibuvir, and LSN2424100. These chemical inhibitors exert their effects as either selective antagonists or dual antagonists, strategically targeting Orexin R-2 and influencing its activity, consequently disrupting downstream cellular responses. For instance, TCS-OX2-29 operates as a selective antagonist by competing with endogenous orexin for binding to Orexin R-2. This competition prevents the activation of the receptor and subsequently disrupts the downstream signaling cascades mediated by Orexin R-2. Dual antagonists such as Suvorexant and Almorexant demonstrate a broader impact on orexin signaling pathways. By modulating these pathways, these dual antagonists effectively influence the activity of Orexin R-2 and interrupt downstream cellular responses mediated by orexin receptors. This dual modulation provides a more comprehensive approach to Orexin R-2 inhibition, showcasing the versatility of chemical inhibitors in regulating the complex network of orexin signaling. The detailed understanding of the specific biochemical and cellular pathways influenced by these inhibitors offers valuable insights into the pharmacological modulation of Orexin R-2. Further research into this class of chemicals holds the potential to deepen our understanding of orexin receptor regulation, unraveling the intricacies of the molecular processes involved in sleep-wake regulation and other physiological functions controlled by Orexin R-2.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

TCS OX2 29

372523-75-6sc-204329
sc-204329A
10 mg
50 mg
$185.00
$781.00
(2)

TCS OX2 29 functions as a selective agonist for the orexin receptor 2, showcasing a unique ability to stabilize receptor conformations that promote activation. Its intricate molecular design facilitates specific hydrophobic interactions, enhancing receptor affinity and triggering distinct intracellular signaling pathways. The compound's kinetic profile indicates rapid receptor engagement, while its lipophilic nature supports efficient membrane permeability, optimizing its interaction dynamics within cellular environments.

TCS 1102

916141-36-1sc-361375
sc-361375A
10 mg
50 mg
$153.00
$643.00
(0)

TCS 1102 acts as a selective antagonist for the orexin receptor 2, exhibiting a unique capacity to disrupt receptor-ligand interactions. Its structural characteristics allow for specific electrostatic interactions that hinder receptor activation, effectively modulating downstream signaling pathways. The compound's kinetic behavior reveals a slow dissociation rate from the receptor, contributing to prolonged effects. Additionally, its polar nature influences solubility and distribution within biological systems, impacting its overall interaction profile.

EMPA

680590-49-2sc-498747
10 mg
$380.00
(0)

Dual orexin receptor antagonist with preference for Orexin R-2. EMPA modulates orexin signaling, influencing the activity of Orexin R-2 and disrupting downstream cellular responses.

SB-334867

792173-99-0sc-507323
10 mg
$207.00
(0)

Selective antagonist of Orexin R-1 and R-2, specifically inhibiting orexin-induced responses. SB-334867 interferes with the binding of orexin to Orexin R-2, blocking receptor activation and subsequent cellular effects.

Almorexant

871224-64-5sc-507322
10 mg
$330.00
(0)

Dual orexin receptor antagonist, with affinity for both Orexin R-1 and R-2. Almorexant modulates orexin signaling pathways, influencing the activity of Orexin R-2 and interrupting downstream cellular responses mediated by orexin receptors.

JNJ 10397049

708275-58-5sc-491320
1 mg
$189.00
1
(0)

Potent and selective antagonist of Orexin R-2, inhibiting orexin-induced responses. JNJ-10397049 competitively binds to Orexin R-2, preventing receptor activation and downstream signal transduction.

Filorexant

1088991-73-4sc-507325
10 mg
$380.00
(0)

Dual orexin receptor antagonist with affinity for Orexin R-2. Filorexant modulates orexin signaling pathways, influencing the activity of Orexin R-2 and disrupting downstream cellular responses mediated by orexin receptors.