CERC-501

Overview
Catalog #	bs-6542c-2mg-solid
Product Name	CERC-501
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 418.5 Formula: C26 H27 F N2 O2 CAS Number: 1174130-61-0 InChi Key: ZHPMYDSXGRRERG-DEOSSOPVSA-N InChi: InChI=1S/C26H27FN2O2/c1-17-12-18(2)14-21(13-17)24-4-3-11-29(24)16-19-5-8-22(9-6-19)31-25-10-7-20(26(28)30)15-23(25)27/h5-10,12-15,24H,3-4,11,16H2,1-2H3,(H2,28,30)/t24-/m0/s1 Smiles: CC1=CC(=CC(C)=C1)[C@@H]1CCCN1CC1C=CC(=CC=1)OC1C=CC(=CC=1F)C(N)=O Purity: 98.0 Solubility: Soluble in DMSO Appearance: Solid Power Shelf Life: 1.0 years
Description	CERC-501, also known as JNJ-67953964, LY-2456302 and Aticaprant, is a potent, selective, short-acting antagonist of the κ-opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR). Aticaprant is under development for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence. Aticaprant has been found to dose-dependently block fentanyl-induced miosis at 25 mg and 60 mg in humans (with minimal to no blockade at doses of 4 to 10 mg), indicating that the drug significantly occupies and antagonizes the MOR at a dose of at least 25 mg but not of 10 mg or less.