5-[3-[4-(2-Bromo-5-fL
MK-8245
CAS: 1030612-90-8
Molecular Formula: C17H16BrFN6O4
5-[3-[4-(2-Bromo-5-fL - Names and Identifiers
5-[3-[4-(2-Bromo-5-fL - Physico-chemical Properties
| Molecular Formula | C17H16BrFN6O4 |
| Molar Mass | 467.25 |
| Density | 1.82 |
| Boling Point | 698.3±65.0 °C(Predicted) |
| pKa | 2.85±0.10(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Use | MK-8245 is a stearoyl-CoA desaturase (SCD)(stearoyl-CoA desaturase) inhibitor that targets the liver. When it acts on human SCD1, the IC50 is 1 nM, and when it acts on rat and mouse SCD1, the IC50 is 3 nM. It has anti-diabetic and anti-hyperlipidemia effects. Phase 2. |
| In vitro study | MK-8245 is a phenoxypiperidine isoxazole derivative that has been used as a potent selective inhibitor of SCD in the liver. MK-824 contains a tetrazolium acetate group with key functions of OATPs recognition and liver targeting. MK-8245 for human, rat and mouse SCD1 have similar efficacy, for human SCD1,IC50 value is 1 nM, for rat and mouse SCD1,IC50 value is 3 nM. MK-8245 in the experiment of rat liver cells containing functional active OATPs, SCD was significantly inhibited, IC50 was 68 nM, but the IC50 was ~ 1 M in the experiment of HepG2 cells lacking active OATPs. In HepG experiments, MK-8245 was highly selective for Delta -5 and Delta -6 desaturases. MK-8245 is a phenoxypiperidine isoxazole derivative that has been used as a potent selective inhibitor of SCD in the liver. MK-824 contains a tetrazolium acetate group with key functions of OATPs recognition and liver targeting. MK-8245 for human, rat and mouse SCD1 have similar efficacy, for human SCD1,IC50 value is 1 nM, for rat and mouse SCD1,IC50 value is 3 nM. MK-8245 in the experiment of rat liver cells containing functional active OATPs, SCD was significantly inhibited, IC50 was 68 nM, but the IC50 was ~ 1 M in the experiment of HepG2 cells lacking active OATPs. In HepG experiments, MK-8245 was highly selective for Delta -5 and Delta -6 desaturases. |
| In vivo study | MK-8245 oral administration to mice, rats, dogs, and macaques showed that MK-8245 of the primary site of action was the liver, and rarely to tissues associated with potential adverse effects. The effect was dose-dependent by applying MK-8245 to eDIO mice and then carrying out sugar screening to increase the sugar scavenging power with an ED50 of 7 mg/kg. MK-8245 oral administration to mice, rats, dogs, and macaques showed that MK-8245 of the primary site of action was in the liver and rarely to tissues associated with potential adverse effects. The effect was dose-dependent by applying MK-8245 to eDIO mice and then carrying out sugar screening to increase the sugar scavenging power with an ED50 of 7 mg/kg. |
5-[3-[4-(2-Bromo-5-fL - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.14 ml | 10.701 ml | 21.401 ml |
| 5 mM | 0.428 ml | 2.14 ml | 4.28 ml |
| 10 mM | 0.214 ml | 1.07 ml | 2.14 ml |
| 5 mM | 0.043 ml | 0.214 ml | 0.428 ml |
Last Update：2024-01-02 23:10:35
5-[3-[4-(2-Bromo-5-fL - Reference Information
| biological activity | MK-8245 is a stearoyl-CoA desaturase (SCD)(stearoyl-CoA desaturase) inhibitor that targets the liver. When acting on human SCD1, IC50 is 1 nM, and when acting on rat and mouse SCD1, IC50 is 3 nM, which has anti-diabetic and anti-hyperlipidemia effects. Phase 2. MK-8245 is a stearoyl-CoA desaturase (SCD)(stearoyl-CoA desaturase) inhibitor that targets the liver. When it acts on human SCD1, the IC50 is 1 nM, and when it acts on rat and mouse SCD1, the IC50 is 3 nM, which has anti-diabetic and anti-hyperlipidemia effects. Phase 2. |
| In vitro study | MK-8245 is a phenoxypiperidine isoxazole derivative, which has been used as an effective liver SCD selective inhibitor. The MK-824 contains tetrazolazole acetic acid group, and its key functions are OATPs recognition and liver targeting. MK-8245 has similar effects on human, rat and mouse SCD1, acting on human SCD1 with IC50 value of 1 nM, acting on rat and mouse SCD1 with IC50 value of 3 nM. MK-8245 acts on rat hepatocytes containing functionally active OATPs, significantly inhibiting SCD with IC50 of 68 nM, but when acting on HepG2 cells lacking active OATPs, IC50 is ~ 1 μM. In the HepG experiment, MK-8245 action on Δ-5 and Δ-6 desaturases is highly selective. MK-8245 is a phenoxypiperidine isoxazole derivative, which has been used as an effective selective inhibitor of liver SCD. The MK-824 contains tetrazolazole acetic acid group, and its key functions are OATPs recognition and liver targeting. MK-8245 has similar effects on human, rat and mouse SCD1, acting on human SCD1 with IC50 value of 1 nM, acting on rat and mouse SCD1 with IC50 value of 3 nM. MK-8245 acts on rat hepatocytes containing functionally active OATPs, significantly inhibiting SCD with IC50 of 68 nM, but when acting on HepG2 cells lacking active OATPs, IC50 is ~ 1 μM. In the HepG experiment, the MK-8245 is highly selective for the Δ-5 and Δ-6 desaturases. |
| in vivo studies | MK-8245 oral administration to mice, rats, dogs, and rhesus monkeys showed that the main site of action of the MK-8245 was the liver, but rarely on tissues related to potential adverse reactions. MK-8245 acts on eDIO mice, and then sugar screening is carried out to improve sugar scavenging capacity. ED50 is 7 mg/kg, which is dose-dependent. MK-8245 oral administration to mice, rats, dogs, and rhesus monkeys showed that the main site of action of the MK-8245 is the liver, but rarely acts on tissues related to potential adverse reactions. MK-8245 acts on eDIO mice, and then sugar screening is carried out to improve sugar scavenging capacity. ED50 is 7 mg/kg, which is dose-dependent. |
| features | MK-8245 is a potent liver-targeting SCD inhibitor and does not affect SCD enzymes in skin and eye tissues compared to other SCD inhibitors. |
| target | TargetValue SCD1 (human) 1 nM SCD1 (rat) 3 nM SCD1 (mouse) 3 nM |
| Target | Value |
| SCD1 (human) | 1 nM |
| SCD1 (rat) | 3 nM |
| SCD1 (mouse) | 3 nM |
Last Update：2024-04-09 02:00:01
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CAS: 1030612-90-8
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Product Name: MK-8245 Visit Supplier Webpage Request for quotation
CAS: 1030612-90-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1030612-90-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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