Orexin Receptors

Cat. No.

A12786

CAS No.

249889-64-3

SB 334867

SB 334867 is a selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.

Cat. No.

A12651

CAS No.

380899-24-1

SB-649868

SB-649868 is an orexin receptor antagonist in development by GlaxoSmithKline.

Cat. No.

A12685

CAS No.

1505484-82-1

Nemorexant

Synonyms: ACT-541468

Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.

Cat. No.

A13168

CAS No.

1088991-73-4

MK-6096 (Filorexant)

Synonyms: Filorexant

MK6096, also known as filorexant, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (170 receptors and enzymes.

Cat. No.

A13439

CAS No.

916141-36-1

TCS 1102

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).

Cat. No.

A14286

CAS No.

913358-93-7

Almorexant HCl

Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.

Cat. No.

A11567

CAS No.

288150-92-5

SB-408124

SB-408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.

Cat. No.

A12401

CAS No.

1191044-58-2

GSK1059865

GSK1059865 is a potent orexin 1 receptor antagonist.

Cat. No.

A12503

CAS No.

871224-64-5

Almorexant

Synonyms: Act-078573

Almorexant(ACT078573) 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.

Cat. No.

A12633

CAS No.

1224846-01-8

MK-3697

MK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists.

Cat. No.

A13778

CAS No.

1354039-86-3

ACT-335827

ACT-335827 is a selective orexin receptor 1 antagonist.

Cat. No.

A14104

CAS No.

708275-58-5

JNJ-10397049

JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R).

Cat. No.

A15231

CAS No.

1431697-90-3

SB-408124 HCl

Synonyms: SB 408124 Hydrochloride

SB408124 Hcl 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.

Cat. No.

A15233

CAS No.

483313-22-0

SB-674042

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.

Cat. No.

A16360

CAS No.

1207253-08-4

MK-1064

MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for potential treatment of insomnia.

Cat. No.

A16695

CAS No.

792173-99-0

SB-334867 free base

Synonyms: SB334867A free base

SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

Cat. No.

A17136

CAS No.

1610882-30-8

TCS-OX2-29 HCl

Synonyms: TCSOX229

TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base)

Cat. No.

A19422

CAS No.

1293281-49-8

Seltorexant

Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R).

Cat. No.

A20457

CAS No.

372523-75-6

TCS-OX2-29

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

Cat. No.

A21276

CAS No.

1373765-19-5

IPSU

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

Cat. No.

A62705

CAS No.

680590-49-2

EMPA

EMPA is a selective and reversible antagonist of the orexin OX2 receptor. It demonstrates high-affinity binding, with KD values of 1.1 nM for human and 1.4 nM for rat OX2-HEK293 membranes. This compound is valuable for research into the role of orexin signaling in various physiological processes and related disorders.

Cat. No.

A62707

CAS No.

1517965-94-4

Vornorexant

Synonyms: ORN-0829; TS-142

Vornorexant is a potent antagonist of both the OX1R and OX2R receptors, exhibiting IC50 values of 1.05 nM and 1.27 nM, respectively. This compound is primarily utilized in studies focused on sleep physiology and insomnia, demonstrating significant sleep-promoting effects in vivo. It serves as a valuable tool for researchers investigating the pathophysiology of sleep disorders and the therapeutic potential of orexin receptor modulation.

Cat. No.

A62710

CAS No.

1293284-49-7

Seltorexant hydrochloride

Synonyms: JNJ-42847922 hydrochloride

Seltorexant hydrochloride is a selective antagonist of the orexin-2 receptor (OX2R), exhibiting high affinity characterized by pKi values of 8.0 and 8.1 in human and rat OX2R, respectively. This compound is capable of permeating the blood-brain barrier and effectively occupies OX2R binding sites in the rat brain. Seltorexant hydrochloride is valuable for research applications focused on sleep disorders and the modulation of wakefulness, making it a pertinent tool in neuroscience studies.

Cat. No.

A62713

CAS No.

1361321-96-1

ACT-462206

ACT-462206 is a potent dual antagonist of the Orexin 1 and Orexin 2 receptors, demonstrating IC50 values of 60 nM and 11 nM, respectively. This orally active compound exhibits favorable brain penetration, making it suitable for research into insomnia, anxiety disorders, and addiction. Its targeted mechanism allows for exploration of orexin signaling pathways and their role in regulating sleep and stress responses.

Cat. No.

A62716

CAS No.

1803557-42-7

CVN766

CVN766 is an orally active orexin-1 receptor antagonist, exhibiting an IC50 of 8 nM for OX1R and greater than 10 μM for OX2R, indicating selectivity. This compound demonstrates effective blood-brain barrier permeability, making it suitable for neurological studies. CVN766 is primarily utilized in research related to schizophrenia, providing insights into the role of orexin receptors in neuropsychiatric disorders.