化合物 MK-3903|T5187|TargetMol

MK-3903
1219737-12-8

询价 1removed 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 MK-3903

英文名称：: MK-3903

CAS号：: 1219737-12-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.63%

产品类别：: 抑制剂

货号：: T5187

Product Introduction

Bioactivity

Name	MK-3903
Description	MK-3903 is a potent and selective AMPK activator (EC50: 8 nM).
Kinase Assay	Briefly, the AMPK complex of interest is appropriately diluted in AMPK reaction buffer and incubated at room temperature for 30 min to yield pAMPK. Then, MK-3903 and pAMPK are pre-incubated by adding appropriately diluted MK-3903 in DMSO (1.2 μL total) to the reaction buffer containing pAMPK (15 μL per well), the plate is vortexed briefly and then incubated at room temperature for 30 min. The plate is sealed and incubated at room temperature for 60 min, at which time the reaction is stopped by the addition of quench buffer. EC50s and %activation parameters are calculated from %product vs. activator concentration plots.
Animal Research	DIO mice at 17 weeks of age are used in this study. Mice are conditioned to dosing with vehicle (5% Tween 80, 0.25% methylcellulose, 0.02% SDS) at 5 mL/kg BID for 5 days. At that time, mice are bled, glucose and insulin measured and the animals sorted into treatment groups based on glucose, insulin and body weight. Each group of animals receives the administration of MK-3903 in a vehicle at 3 mg/kg, 10 mg/kg, 30 mg/kg, or vehicle alone for 12-day BID. Another group of mice receiving MK-3903 with the vehicle at 30 mg/kg for 12-day QD is included as well. Food intake and body weight are measured daily.
In vitro	MK-3903在12种磷酸化AMPK（pAMPK）复合体中激活了10种，其EC50值范围为8至40nM。MK-3903对pAMPK5具有部分激活作用（最大36%），但不激活pAMPK6。MK-3903在LLC-PK1细胞中显示出低渗透性，并且是人肝摄取转运蛋白OATP1B1和OATP1B3（有机阴离子转运蛋白）的底物。MK-3903与前列腺素DP2（CRTH2）受体有中等程度的结合能力（IC50: 1.8 μM），但在含有10%人血清的情况下不绑定（结合IC50>86 μM）。
In vivo	MK-3903在C57BL/6小鼠、SD大鼠和比格犬中的药代动力学特征表现为中等的系统性血浆清除率（5.0至13 mL/min/kg）、稳态分布容积为0.6至1.1 L/kg，以及终末半衰期约为2小时。在高果糖饲料喂养的db/+小鼠中，MK-3903的急性口服给药（3、10和30 mg/kg）显著抑制了所有三个剂量的肝脏脂肪酸合成（FAS）。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : Insoluble DMSO : 50 mg/mL (109.91 mM) Ethanol : Insoluble
Keywords	MK3903 \| AMPK \| AMP-activated protein kinase \| inhibit \| Inhibitor \| MK-3903
Inhibitors Related	Chitosan oligosaccharide \| A-769662 \| Doxorubicin hydrochloride \| Metformin \| AICAR \| Buformin hydrochloride \| Phenformin hydrochloride \| HTH-01-015 \| Metformin hydrochloride \| AMPK activator 4 \| Adenosine monophosphate \| Methyl cinnamate
Related Compound Libraries	Neuroprotective Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Diabetic Compound Library \| Anti-Aging Compound Library \| Anti-Liver Cancer Compound Library \| Anti-Hypertension Compound Library \| Antioxidant Compound Library \| Glycometabolism Compound Library

MK 3903|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
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