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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 22 mg/mL|
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, et al. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. PMID: 25248679.
|Related OX Receptor Products|
MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for the research of insomnia.
SB-649868 is a selective orally active orexin (OX) receptor antagonist with pKi values of 9.4 and 9.5 at the OX1 and OX2 receptor, respectively.
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
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.
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