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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.
| Molecular Weight | 447.51 |
| Formula | C23H21N5O3S |
| CAS Number | 1224846-01-8 |
| Solubility (25°C) | DMSO 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related OX Receptor Products |
|---|
| MK-6096
MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R. |
| Almorexant
Almorexant is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. |
| SB408124
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
| 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). |
| SB-334867 hydrochloride
SB-334867 hydrochloride is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. |
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