| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell lines | podocytes |
Preparation Method | 1.75 × 104podocytes per well were seeded in 24-well microplates for 7 days. Baseline OCR was measured in control (vehicle) or INT-777 (10 μM) treated cells. To determine fatty acid β-oxidation cells were treated with BAS-complexed palmitate (0.5 mM) followed by treatment with control or INT-777 (10 μM). |
Reaction Conditions | 10 μM; 7 days |
Applications | INT-777 increased mitochondrial oxygen consumption rate and suppressed mitochondrial ROS production as determined by Mito Sox staining. INT-777 also induced increases in mitochondrial p-AMPK and PGC-1α protein. |
Animal models | Sprague-Dawley rats |
Preparation Method | A total volume of 30 μL vehicle (10% dimethyl sulfide) or INT-777 at three different doses (10 μg/kg, 30 μg/kg, and 90 μg/kg) were administered into the right and left nares, alternating 10 μL in one naris per 5 minutes. H89 was diluted in 10% dimethyl sulfide (DMSO) and was administrated by intraperitoneally (i.p.) at 1 h before SAH. |
Dosage form | 10 μg/kg, 30 μg/kg, and 90 μg/kg; Intranasal |
Applications | The medium (30μg/kg) and high (90μg/kg) doses of INT-777 administration significantly improved the neurological deficits on modified Garcia test and beam balance test at 24 h after SAH compared with the vehicle group. |
| 产品描述 | INT-777 is a novel specific semisynthetic TGR5 agonist used for alleviating cardiomyocyte injury and improving cognitive impairment and synaptic dysfunction in mice model of AD.[1][2] In vitro, INT-777 induced a dose-dependent (10 μM to 60 μM) decrease in Isc, when INT-777 added on the serosal side of seromuscular stripped distal colon segments in Ussing chambers.[5]In vitro experiment it shown that treatment with 25 μm of INT-777 for 48 h in αTC1-6 cells as well as in mouse and human islets under high glucose conditions obviously increased PC1 mRNA. However, INT-777 (25 μm) had no effect on PC1 mRNA in cells exposed to low glucose conditions.[6]In vitro, combination 100 ng/ml LPS with treatment of 30 μM INT-777 dramatically decreased the transient increase in mRNA levels for Tnfα, monocyte chemoattractant protein-1 (Mcp-1), Il-6 and Il-1β in macrophages.[7] In vivo efficacy test it indicated that treatment with 30μg/kg of INT-777 dramatically reduced NLRP3-ASC inflammasome activation in microglia, decreased brain edema and neuroinflammation, resulted in improved short-term neurobehavioral functions at 24 h after subarachnoid hemorrhage.[3]In vivo study it suggested that mice were treated with 1.5 or 3.0 μg/mouse INT-777, single intracerebroventricular (i.c.v.) injection of LPS obviously induced mouse behavioral impairments in Morris water maze, novel object recognition, and Y-maze avoidance tests were ameliorated.[7]. References: |
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