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Results for "

orexin receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Orexin Receptor (OX Receptor) (29) Apoptosis (2) Calcium Channel (2) Caspase (2) Isotope-Labeled Compounds (1) Prostaglandin Receptor (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (2) Endocrinology (14) Metabolic Disease (2) Neurological Disease (23)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Orexin Receptor (OX Receptor)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136922

Orexin receptor antagonist 2	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin receptor antagonist 2 (compound 30) is a potent **orexin receptor** antagonist with pK_is of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia .

HY-137093

Orexin receptor antagonist 3 1 Publications Verification	Orexin Receptor (OX Receptor)	Metabolic Disease
Orexin receptor antagonist 3 (example 216) is an **orexin receptor** antagonist, which is extracted from the patent WO2011050198A1 .

HY-108683

ACT-335827	Orexin Receptor (OX Receptor)	Neurological Disease
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC₅₀ values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders .

HY-147294

Nivasorexant ACT-539313	Orexin Receptor (OX Receptor)	Neurological Disease
Nivasorexant is a potent **orexin receptor** antagonist .

HY-101534

GSK1059865	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
GSK1059865 is a potent **orexin 1 receptor** antagonist.

HY-101834

ACT-462206	Orexin Receptor (OX Receptor)	Others
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .

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-123737

MK-8133	Orexin Receptor (OX Receptor)	Neurological Disease
MK-8133 is an *orexin-2* receptor antagonist. MK-8133 can be used in the study of insomnia .

HY-113555

DORA 42	Orexin Receptor (OX Receptor)	Neurological Disease
DORA 42 is a dual orexin 1 and **orexin 2 receptor** antagonist with sleep efficacy in rats. DORA 42 is promising for research of insomnia .

HY-10805S

Almorexant-13C,d3 ACT 078573-¹³C,d₃	Isotope-Labeled Compounds 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-172436

Rocavorexant	Orexin Receptor (OX Receptor)	Neurological Disease
Rocavorexant is the antagonist for **orexin-1 receptor** with pIC₅₀ of 9.1 for human OX1 (while pIC₅₀ for human OX2 is 6.0) .

HY-152843

Fazamorexant YZJ-1139	Orexin Receptor (OX Receptor)	Neurological Disease
Fazamorexant (YZJ-1139) is a potent **orexin receptor** antagonist. Fazamorexant can be used for insomnia research .

HY-12301

MK-3697	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.

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-10805A

Almorexant hydrochloride 4 Publications Verification ACT 078573 hydrochloride	Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis	Neurological Disease Endocrinology Cancer
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 Ca ²⁺ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .

HY-10805

Almorexant 4 Publications Verification ACT 078573	Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis	Neurological Disease Endocrinology Cancer
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 Ca ²⁺ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .

HY-100452A

TCS-OX2-29 hydrochloride OX2R antagonist	Orexin Receptor (OX Receptor)	Endocrinology Cancer
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-100452

TCS-OX2-29 2 Publications Verification	Orexin Receptor (OX Receptor)	Endocrinology Cancer
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-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 blood-brain barrier penetrability and moderate bioavailability in rats .

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_is of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor .

HY-109012

Seltorexant 1 Publications Verification 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-149014

OX2R-IN-1	Orexin Receptor (OX Receptor)	Neurological Disease
OX₂R-IN-1 (compound 15) is a low cytotoxicity profile OX₂R-IN-1 antagonist (a potential OX2R binder) with an IC₅₀ value of 484 μM. OX₂R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .

HY-10898

SB-674042 1 Publications Verification	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-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-10896

JNJ-10397049 1 Publications Verification	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-162235

CVN766	Orexin Receptor (OX Receptor)	Cardiovascular Disease
CVN766 is an orally active inhibitor of **orexin 1 receptor** antagonist with blood-brain permeability with the IC₅₀ values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia .

HY-108682

EMPA Maximum Cited Publications 7 Publications Verification	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-10895

SB-334867 5+ Cited Publications 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-114761

Prostaglandin F2α dimethyl amine	Prostaglandin Receptor	Cardiovascular Disease
Prostaglandin F2α dimethyl amine is a Prostaglandin F2α (HY-12956) derivative. Prostaglandin F2α dimethyl amine is an antagonist for Prostaglandin F receptor (FP) . Prostaglandin F2α dimethyl amine blocks the cardiovascular responses induced by orexin and Arachidonic acid (HY-109590) .

HY-10895A

SB-334867 free base 5+ Cited Publications 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 .

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.

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