|Targets||Orexin Receptor (OX Receptor)|
|Description||MK3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. MK-3697 is also the third insomnia product, currently being developed by Merck. MK-3697 has Ki = 0.95 nM. Orexin receptor antagonists have demonstrated clinical utility for the treatment of insomnia. In vivo tests results on MK-3697 demonstrated improved stability and TDI profiles as well as excellent sleep efficacy across species.|
|Appearance||white solid powder|
|Synonyms||MK-3697; MK3697; MK 3697.|
MK3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. MK-3...
SB-649868 is a novel, orally active dual orexin receptor antagonist of orexin(OX)1 and OX2 receptor (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively),...
Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the tre...
TCS 1102 is a potent, dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively. It is a poor substrate for P-glycop...
JNJ-10397049 is a selective orexin-2 receptor (OX2) antagonist. pIC50 is 7.4 for chimeric OX2 receptors/ pKB values are 5.9 for OX1 and 8.5 for OX2 receptors re...
SB-674042 is potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM), by binding with high affinity to OX1R and mediates intracellular ca...
SB-408124 (Hydrochloride) is the hydrochloride salt form of SB-408124. SB-408124 is a selective antagonist of OX1 (for human OX1 Kb= 21.7nM; for human OX2 Kb=14...
SB-334867, with sedative and anorectic effects, it is the first non-peptide selective antagonist of orexin receptor subtype OX1 (pKb= 7.2) with 50 -fold selecti...
IPSU is a selective, orally available and brain penetrant OX2 receptor antagonist (pKi= 7.85) with 6-fold selectivity over OX1 receptors.
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
Orexin 2 Receptor Agonist
N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide is an orexin 2 receptor agonist that is potentially for...
TCS-OX2-29, also known as TCSOX229, is a selective OX2 receptor antagonist (IC50 = 40 nM, pKi = 7.5) with >250-fold selectivity for hOX2R compared with hOX1R (I...
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...
Lemborexant, an orexin OX1/OX2 receptors antagonist, has been found to be effective against insomnia and is just planed a Phase III trail by Eisai.
Almorexant HCl 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, re...
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 ...