Summary of project PR000760

This data is available at the NIH Common Fund's National Metabolomics Data Repository (NMDR) website, the Metabolomics Workbench,, where it has been assigned Project ID PR000760. The data can be accessed directly via it's Project DOI: 10.21228/M8FH6C This work is supported by NIH grant, U2C- DK119886.


Project ID: PR000760
Project DOI:doi: 10.21228/M8FH6C
Project Title:Antidiabetic and cardiovascular beneficial effects of a liver-localized mitochondrial uncoupler
Project Summary:Inducing mitochondrial uncoupling (mUncoupling) is an attractive therapeutic strategy for treating metabolic diseases because it leads to calorie-wasting by reducing the efficiency of oxidative phosphorylation (OXPHOS) in mitochondria. Here we report a safe mUncoupler, OPC-163493, which has unique pharmacokinetic characteristics. OPC-163493 shows a good bioavailability upon oral administration and primarily distributed to specific organs: the liver and kidneys, avoiding systemic toxicities. It exhibitsinsulin-independent antidiabetic effects in multiple animal models of type I and type II diabetes and antisteatotic effects in fatty liver models. These beneficial effects can be explained by the improvement of glucose metabolism and enhancement of energy expenditure by OPC-163493 in the liver. Moreover, OPC-163493 treatment lowered blood pressure, extended survival, and improved renal function in the rat model of stroke/hypertension, possibly by enhancing NO bioavailability in blood vessels and reducing mitochondrial ROS production. OPC-163493 is a liver-localized/targeted mUncoupler that ameliorates various complications of diabetes.
Institute:Otsuka Pharmaceutical Co., Ltd.
Last Name:Kanemoto
First Name:Naohide
Address:463-10 Kagasuno Kawauchi-cho, Tokushima, Tokusima, 770-0865, Japan

Summary of all studies in project PR000760

Study IDStudy TitleSpeciesInstituteAnalysis
(* : Contains Untargted data)
(* : Contains raw data)
ST001135 Different dose exposure of OPC-163493 on HepG2 cells (part-I) Homo sapiens Otsuka Pharmaceutical Co., Ltd. MS 2019-03-06 1 8 Uploaded data (894.3K)
ST001136 Metabolme analysis of OPC-163493 on the Liver of ZDF rats (part-II) Rattus norvegicus Otsuka Pharmaceutical Co., Ltd. MS 2019-03-06 1 24 Uploaded data (919.5K)