MK-8245 NEW
| Price | $33 | $47 | $97 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: MK-8245 | CAS No.: 1030612-90-8 |
| Purity: 99% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | MK-8245 |
| 描述 | MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function. |
| 激酶實(shí)驗(yàn) | High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program. |
| 體外活性 | In mice, rats, dogs, and cynomolgus monkeys, the primary site of action for MK-8245 (p.o.) is the liver, displaying minimal efficacy in tissues associated with potential adverse reactions. In eDIO mice, MK-8245 demonstrates a dose-dependent effect on glucose screening, enhancing glucose clearance (ED50: 7 mg/kg). |
| 體內(nèi)活性 | In experiments conducted on rat liver cells exhibiting functional activity of OATPs, MK-8245 demonstrated a potent inhibitory effect on SCD, with an IC50 of 68 nM. However, in experiments with HepG2 cells, which lack active OATPs, the compound was less effective, showing an IC50 of 1 μM. In HepG experiments, MK-8245 displayed high selectivity towards Δ-5 and Δ-6 desaturases. MK-8245 contains a tetrazole acetic acid group, endowing it with the capability for OATP recognition and liver-targeting functions. |
| 存儲條件 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 86 mg/mL (184.1 mM) |
| 關(guān)鍵字 | Inhibitor | Stearoyl-CoA Desaturase (SCD) | MK-8245 | MK8245 | MK 8245 | inhibit |
| 相關(guān)產(chǎn)品 | Disulfiram | Methotrexate | ALDH1A3-IN-3 | Rotenone | Mycophenolate Mofetil | Ribavirin | 4-Diethylaminobenzaldehyde | Benzyl alcohol | Isomalt | Isoniazid | Sodium Oxamate | Ivosidenib |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | ReFRAME 相關(guān)化合物庫 | 抗肥胖化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 臨床期小分子藥物庫 | 已知活性化合物庫 | 含氟化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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