Product Details
Product Name:
MK8722 |
CAS No.:
1394371-71-1 |
Purity:
99.88% |
Supply Ability:
10g |
Release date:
2024/11/15 |
Product Introduction
Bioactivity
名稱 | MK8722 |
描述 | MK8722 is an effective and systemic activator of pan-AMPK. |
體外活性 | MK8722 is an effective, direct, allosteric activator of all 12 mammalian AMPK complexes. pAMPK activation by maximal AMP plus MK8722 is synergistic, demonstrating that the agents act at distinct sites. MK8722 activates pAMPK complexes with increased potency and magnitude versus AMP (EC50: ~1 to 60 nM) and increased activation by factors of ~4 to 24. Although MK8722 exhibits a higher affinity for β1-containing (~1 to 6 nM) versus β2-containing (~15 to 63 nM) pAMPK complexes, it is the most potent activator of β2 complexes reported to date . |
體內(nèi)活性 | MK8722(once-daily)administration, causes dose-dependent lowering of ambient blood glucose. Chronic MK8722 dosing in mice also increases muscle Glut4 protein levels, possibly contributing to efficacy. Chronic antihyperglycemic efficacy of MK8722 is evaluated in db/db mice (a leptin receptor-deficient T2DM model). Glucose reductions after MK8722 treatment (30 mpk/day) are comparable to those observed with the PPARγ agonist BRL49653 (3 mpk/day), on treatment day 12. Dose-dependent enhances in tissue pACC are maintained throughout the dosing period. Chronic efficacy, without tachyphylaxis, is also observed in additional dysmetabolic and diabetic rodent models. In all cases, efficacy is associated with trough MK8722 plasma levels comparable to the concentrations required to acutely stimulate skeletal muscle glucose uptake. The glucose-lowering action of MK8722 manifests without significant effects on body weight . |
存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (111.14 mM), Sonication is recommended.
|
關(guān)鍵字 | AMP-activated protein kinase | inhibit | Inhibitor | MK-8722 | AMPK | MK8722 | MK 8722 |
相關(guān)產(chǎn)品 | Phenformin hydrochloride | AICAR | Doxorubicin hydrochloride | Adenosine monophosphate | Metformin | Methyl cinnamate | A-769662 | Metformin hydrochloride | Chitosan oligosaccharide | Buformin hydrochloride | HTH-01-015 | AMPK activator 4 |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗抑郁癥化合物庫(kù) | 激酶抑制劑庫(kù) | 自噬庫(kù) | 細(xì)胞焦亡化合物庫(kù) | 神經(jīng)保護(hù)化合物庫(kù) | 干細(xì)胞分化化合物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 神經(jīng)元分化化合物庫(kù) |
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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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |