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Orexin Receptor (OX Receptor)

" in MCE Product Catalog:

By Targets:	Orexin Receptor (OX Receptor) (31) Apoptosis (3) Calcium Channel (2) Caspase (2)
By Research Areas:	Cancer (5) Endocrinology (17) Metabolic Disease (1) Neurological Disease (27)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Targets Recommended: Orexin Receptor (OX Receptor)

Cat. No.	Product Name	Target	Research Areas

HY-P1349

Orexin B, rat, mouse Rat Orexin B; Orexin B (mouse)	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-P1339

Orexin B, human Human Orexin B	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-146517

Orexin receptor antagonist 4	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin receptor antagonist 4 is potent and selective **orexin 2 receptor (OX2R) antagonist with an IC₅₀** of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC₅₀ of 295 nM) (WO2018206959A1; example 1).

HY-P1339A

Orexin B, human TFA Human Orexin B TFA	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human (TFA) is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-10805S

Almorexant-13C,d3 ACT 078573-¹³C,d₃	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Almorexant-¹³C,d₃ is the ¹³C- and deuterium labeled Almorexant. 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, respectively.

HY-P1349A

Orexin B, rat, mouse TFA Rat Orexin B TFA; Orexin B (mouse) (TFA)	Orexin Receptor (OX Receptor)	Endocrinology Neurological Disease
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.

HY-10806

SB-649868 GSK649868	Orexin Receptor (OX Receptor)	Metabolic Disease Endocrinology
SB-649868 is a potent and selective orally active *orexin* (OX) 1 and *OX₂* receptor antagonist (pK_i =9.4 and 9.5 at the OX₁ and OX₂ receptor, respectively).

HY-100452

TCS-OX2-29	Orexin Receptor (OX Receptor)	Cancer Endocrinology
TCS-OX2-29 is a potent, high affinities and selective **orexin-2 receptor (OX₂R) antagonist with an IC₅₀ value of 40 nM and a pK_I value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX₂ over OX₁**.

HY-100452A

TCS-OX2-29 hydrochloride OX2R antagonist	Orexin Receptor (OX Receptor)	Cancer Endocrinology
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 pK_I value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX₂ over OX₁**.

HY-P1340

[Ala11,D-Leu15]-Orexin B(human)	Orexin Receptor (OX Receptor)	Neurological Disease
[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).

HY-P1340A

[Ala11,D-Leu15]-Orexin B(human) TFA	Orexin Receptor (OX Receptor)	Neurological Disease
[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).

HY-19320

Orexin 2 Receptor Agonist	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.

HY-P1341

OXA(17-33)	Orexin Receptor (OX Receptor)	Neurological Disease
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).

HY-P1341A

OXA(17-33) TFA	Orexin Receptor (OX Receptor)	Neurological Disease
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).

HY-76612

SB-408124 Hydrochloride	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-408124 Hydrochloride is a selective non-peptide **orexin receptor 1 (OX1) receptor antagonist with K_i*s of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.*

HY-10900

TCS 1102	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for *OX2* and *OX1* receptors, respectively. TCS 1102 demonstrates excellent brain peneration and moderate bioavailability in rats.

HY-10898

SB-674042	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-674042 is a potent and selective non-peptide orexin *OX₁* receptor antagonist (K_d=5.03 nM), exhibits 100-fold selectivity for *OX₁* over *OX₂* receptors with IC₅₀ values of 3.76 nM and 531 nM, respectively.

HY-10896

JNJ-10397049	Orexin Receptor (OX Receptor)	Neurological Disease
JNJ-10397049 is a potent and selective **orexin 2 receptor (OX₂R)** antagonist, with a pK_i of 8.3. JNJ-10397049 is 600-fold selective for the OX₂R over the OX₁R.

HY-P3867

Hypocretin (70-98), human	Orexin Receptor (OX Receptor) Apoptosis	Cancer
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor *OX1R* and promotes apoptosis.

HY-137440

Firazorexton
Orexin Receptor (OX Receptor) Neurological Disease

Firazorexton is a potent orexin type 2 receptor (OX2R) agonist (patent WO2019027058A1, example 395).

Firazorexton	Orexin Receptor (OX Receptor)	Neurological Disease
Firazorexton is a potent **orexin type 2 receptor (OX2R)** agonist (patent WO2019027058A1, example 395).

HY-109012

Seltorexant JNJ-42847922	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective **orexin-2 receptor (OX2R) antagonist (pK_i** values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.

HY-108682

EMPA	Orexin Receptor (OX Receptor)	Neurological Disease
EMPA is a high-affinity, reversible and selective **orexin OX₂ receptor** antagonist. [³H]EMPA binds to human and rat OX₂-HEK293 membranes with K_D values of 1.1 and 1.4 nM respectively.

HY-10805A

Almorexant hydrochloride ACT 078573 hydrochloride	Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis	Cancer Endocrinology Neurological Disease
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual **orexin receptor antagonist, with K_d** values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca²⁺ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

HY-10805

Almorexant ACT 078573	Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis	Cancer Endocrinology Neurological Disease
Almorexant (ACT 078573) is an orally active, potent and competitive dual **orexin receptor antagonist, with K_d** values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca²⁺ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

HY-136181A

YNT-185	Orexin Receptor (OX Receptor)	Neurological Disease
YNT-185 is a nonpeptide, selective **orexin type-2 receptor (OX2R) agonist, with EC₅₀**s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models.

HY-136181

YNT-185 dihydrochloride	Orexin Receptor (OX Receptor)	Neurological Disease
YNT-185 dihydrochloride is a nonpeptide, selective **orexin type-2 receptor (OX2R) agonist, with EC₅₀**s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models.

HY-134188

JNJ-54717793	Orexin Receptor (OX Receptor)	Neurological Disease
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 K_i** 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.

HY-106224

Orexin A (human, rat, mouse) Hypocretin-1 (human, rat, mouse)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor *OX1R. Orexin* A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

HY-106224A

Orexin A (human, rat, mouse) (TFA) Hypocretin-1 (human, rat, mouse) (TFA)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor *OX1R. Orexin* A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

HY-10895

SB-334867 SB 334867A	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable **orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i** values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

HY-10895A

SB-334867 free base SB334867A free base	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable **orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i** values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

Cat. No.	Product Name	Target	Research Area

HY-P1349

Orexin B, rat, mouse Rat Orexin B; Orexin B (mouse)	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-P1339

Orexin B, human Human Orexin B	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-P1339A

Orexin B, human TFA Human Orexin B TFA	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human (TFA) is an endogenous agonist at *Orexin* receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-P1349A

Orexin B, rat, mouse TFA Rat Orexin B TFA; Orexin B (mouse) (TFA)	Orexin Receptor (OX Receptor)	Endocrinology Neurological Disease
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.

HY-P1340

[Ala11,D-Leu15]-Orexin B(human)	Orexin Receptor (OX Receptor)	Neurological Disease
[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).

HY-P1340A

[Ala11,D-Leu15]-Orexin B(human) TFA	Orexin Receptor (OX Receptor)	Neurological Disease
[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).

HY-P1341

OXA(17-33)	Orexin Receptor (OX Receptor)	Neurological Disease
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).

HY-P1341A

OXA(17-33) TFA	Orexin Receptor (OX Receptor)	Neurological Disease
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).

HY-P3867

Hypocretin (70-98), human	Orexin Receptor (OX Receptor) Apoptosis	Cancer
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor *OX1R* and promotes apoptosis.

HY-106224

Orexin A (human, rat, mouse) Hypocretin-1 (human, rat, mouse)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor *OX1R. Orexin* A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

HY-106224A

Orexin A (human, rat, mouse) (TFA) Hypocretin-1 (human, rat, mouse) (TFA)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor *OX1R. Orexin* A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

Cat. No.	Product Name

HY-10805S

Almorexant-13C,d3
Almorexant-¹³C,d₃ is the ¹³C- and deuterium labeled Almorexant. 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, respectively.