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GPCR/G Protein OX Receptor

OX Receptor

The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene. Both orexin receptors exhibit a similar pharmacology - the 2 orexin peptides, orexin-A and orexin-B, bind to both receptors and, in each case, agonist binding results in an increase in intracellular calcium levels. However, orexin-B shows a 10-fold selectivity for orexin receptor type 2, whilst orexin-A is equipotent at both receptors.
Cat No. product name
T1913 MK3697 MK-3697, an isonicotinamide small molecule, acts as a potent and selective Orexin 2 receptor antagonist (Ki: 0.95 nM).
T2613 Almorexant Almorexant 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, respec...
T2710 TCS 1102 TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2/3 nM for OX2/1 receptors).
T3177 Orexin 2 Receptor Agonist Orexin 2 Receptor Agonist is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.
T3347 PF-3274167 PF-3274167 is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.
T3722 MK-1064 MK-1064 is a selective orexin 2 receptor antagonist (2-SORA).
T6140 SB-334867 SB-334867 is a selective orexin-1 (OX1) receptor antagonist.
T6155 Almorexant HCl Almorexant HCl (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...
T6658 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 ove...
T4965 TCS-OX2-29 TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1.
T2742 Aloin A Aloin, a natural anthracycline from Aloe vera, is a tyrosinase inhibitor.
TQ0237 Lemborexant Lemborexant (E-2006) is a reversible and orally active dual antagonist of the orexin OX1 and OX2 receptors (IC50s: 6.1 nM and 2.6 nM).
T11186 EMPA EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respecti...
T16328 Nitroaspirin Nitroaspirin is a nitric oxide donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin induces signifi...
T5500 DORA-22 DORA-22 is a dual orexin receptor antagonist, improves mild stress-induced insomnia with minimal effect on memory
MK3697
T1913CAS 1224846-01-8
MK-3697, an isonicotinamide small molecule, acts as a potent and selective Orexin 2 receptor antagonist (Ki: 0.95 nM).
Almorexant
T2613CAS 871224-64-5
Almorexant 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, respec...
TCS 1102
T2710CAS 916141-36-1
TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2/3 nM for OX2/1 receptors).
Orexin 2 Receptor Agonist
T3177CAS 1796565-52-0
Orexin 2 Receptor Agonist is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.
PF-3274167
T3347CAS 900510-03-4
PF-3274167 is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.
MK-1064
T3722CAS 1207253-08-4
MK-1064 is a selective orexin 2 receptor antagonist (2-SORA).
SB-334867
T6140CAS 792173-99-0
SB-334867 is a selective orexin-1 (OX1) receptor antagonist.
Almorexant HCl
T6155CAS 913358-93-7
Almorexant HCl (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...
SB408124
T6658CAS 288150-92-5
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 ove...
TCS-OX2-29
T4965CAS 372523-75-6
TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1.
Aloin A
T2742CAS 1415-73-2
Aloin, a natural anthracycline from Aloe vera, is a tyrosinase inhibitor.
Lemborexant
TQ0237CAS 1369764-02-2
Lemborexant (E-2006) is a reversible and orally active dual antagonist of the orexin OX1 and OX2 receptors (IC50s: 6.1 nM and 2.6 nM).
EMPA
T11186CAS 680590-49-2
EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respecti...
Nitroaspirin
T16328CAS 175033-36-0
Nitroaspirin is a nitric oxide donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin induces signifi...
DORA-22
T5500CAS 1088991-95-0
DORA-22 is a dual orexin receptor antagonist, improves mild stress-induced insomnia with minimal effect on memory