Aticaprant-CERC-501-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAticaprantCat. No.: HY-101718CAS No.: 1174130-61-0Synonyms: CERC-501; LY-2456302分式: CHFNO分量: 418.5作靶点: Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 100 mg/mL (238.95 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3895 mL 11.9474 mL 23.8949 mL5 mM 0.4779 mL 2.3895 mL 4.7790 mL10 mM 0.2389 mL 1.1947 mL 2.3895 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Atica

3、prant (CERC-501)种有效地可渗透中枢神经的kappa opioid受体拮抗剂，Ki值为0.807 nM。IC50 & Target Ki: 0.807 nM (kappa opioid) 1体外研究Aticaprant (CERC-501) binds with high affinity to the human kappa opioid receptor with a 30-fold higher1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEaffinity over the human mu opioid receptor

4、 and 190-fold higher affinity over the human delta opioid receptor.Aticaprant (CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupledreceptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors or ionchannel/transporter binding t

5、argets or the central benzodiazepine binding site 1.体内研究 Aticaprant (CERC-501) has a rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). OralAticaprant (CERC-501) administration selectively and potently occupies central kappa opioid receptors(ED50=0.33 mg/kg), without evidence of mu

6、 or delta receptor occupancy. LY2456302 potently blocks kappa-agonist-mediated analgesia and disruption of prepulse inhibition, without affecting mu-agonist-mediatedeffects at doses 30-fold higher. Aticaprant (CERC-501) produces antidepressant-like effects in the mouseforced swim test and enhances t

7、he effects of imipramine and citalopram. Aticaprant (CERC-501) reducesethanol self-administration in alcohol-preferring rats 1. Aticaprant (CERC-501) alleviates the nicotinewithdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal induced anxiety-relatedbehavior, somatic signs

8、, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment 2.PROTOCOLAnimal Rats: Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO)Administration 1 dose of Aticaprant (CERC-501) to determine the pharmacokinetic para

9、meters. Plasma samples are collectedat 0.08 (IV only), 0.25, 0.5, 1, 2, 4, 8, 12 and 24 h post-dose and analyzed by liquid chromatography coupledto tandem mass spectral detection to determine the concentrations of Aticaprant (CERC-501) 1.Mice: Male mice are administered a single 10 mg/kg PO dose of

10、Aticaprant (CERC-501) to determine thepharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose andanalyzed by LCeMS/MS to determine the concentrations of Aticaprant (CERC-501). The plasma and brainbinding of Aticaprant (CERC-501) is determined by equilibrium di

11、alysis at 1 M 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Neuropharmacology. 2019 Jul 25:107726.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Rorick-Kehn LM, et al. LY2456302 is a novel, potent, orally-bioavaila

12、ble small molecule kappa-selective antagonist with activity in animalmodels predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44.2. Jackson KJ, et al. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302on nicotine withdrawalin mice. Neuropharmacology. 2015 Oct;97:270-4.McePdfHeight Caution