MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

A-769662

CAS No. : 844499-71-4

MCE 站：A-769662

产品活性：A-769662 是一种有效的，可逆的 AMPK 激活剂，EC₅₀ 值为 0.8 μM。

研究领域：Epigenetics  |  PI3K/Akt/mTOR

作用靶点：AMPK

In Vitro: A-769662 is equally potent in activating the baculovirus expressed α1,β1,γ1 recombinant isoform of AMPK (EC₅₀=0.7 μM). A-769662 and A-592107 activate AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC₅₀s. EC₅₀s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 μM, 1.9 μM, or 1.1 μM, respectively. A-769662 activates endogenous AMPK in LKB1-expressing (HEK293) and LKB1-deficient (CCL13) cells. A-769662 allosterically activates AMPK complexes containing γ1 harboring a substitution of arginine residue 298 to glycine (R298G). A-769662 inhibits dephosphorylation of Thr-172 in the mutant γ1-containing complexes to a similar degree as seen in the wild-type complexes. A769662 (300 μM) has toxic effects on MEF cells. A769662 reversibly inhibits the proteasomal activity.

In Vivo: A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange ratio (RER) in the SD rat. There are 33% and 58% reductions of malonyl CoA levels in livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g), respectively. A-769662 (30 mg/kg, b.i.d.) significantly decreases fed plasma glucose (30%-40% reduction), while the lower doses (3 and 10 mg/kg) of A-769662 had no effect on the in diabetic ob/ob mice.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Antioxidants Compound Library  |  Diabetes Related Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Doxorubicin hydrochloride  |  Metformin hydrochloride  |  Dorsomorphin  |  AICAR  |  GSK-690693  |  STO-609  |  Phenformin hydrochloride  |  [6]-Gingerol  |  WZ4003  |  Palmitelaidic Acid  |  Urolithin B  |  GSK621  |  Flufenamic acid  |  Chitosan oligosaccharide  |  Amarogentin  |  7-Methoxyisoflavone  |  Buformin hydrochloride  |  Danthron  |  Ginkgolide C  |  ZLN024 hydrochloride  |  Ampkinone  |  EB-3D  |  Demethyleneberberine  |  Gomisin J  |  Platycodin D  |  Methyl cinnamate  |  Vaccarin

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。