Summary of Study ST001135
This data is available at the NIH Common Fund's National Metabolomics Data Repository (NMDR) website, the Metabolomics Workbench, https://www.metabolomicsworkbench.org, 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.
See: https://www.metabolomicsworkbench.org/about/howtocite.php
Study ID | ST001135 |
Study Title | Different dose exposure of OPC-163493 on HepG2 cells (part-I) |
Study Type | Compound dosage test |
Study Summary | Metabolomics analysis were on 8 samples of HepG2 cells that were treated with compound OPC-163493 (DMSO control, 1, 3, or 10µM; each n=2) exposure for 30 min. |
Institute | Otsuka Pharmaceutical Co., Ltd. |
Last Name | Kanemoto |
First Name | Naohide |
Address | 463-10 Kagasuno Kawauchi-cho Tokushima 771-0192, Japan |
Kanemoto.Naohide@otsuka.jp | |
Phone | 81-03-6717-1400 |
Submit Date | 2019-02-07 |
Analysis Type Detail | LC-MS |
Release Date | 2019-03-06 |
Release Version | 1 |
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Project:
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 |
Email: | Kanemoto.Naohide@otsuka.jp |
Phone: | +81-88-665-2126 |