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My CartCAS：844499-71-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to brown Solid
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| CAS | 844499-71-4 |
| Name | A-769662 |
| Molecular Formula | C20H12N2O3S |
| Molecular Weight | 360.39 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to brown Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD11977269 |
| SMILES | N#CC1C(C2=C(NC1=O)SC=C2C3=CC=C(C4=CC=CC=C4O)C=C3)=O |
| Target Point | AMPK |
| Passage | PI3K/Akt/mTOR;Epigenetics |
| Background | A-769662 is a potent, reversible AMPK activator. |
| Biological Activity | A-769662 是一种有效的，可逆的 AMPK 激活剂，EC50 值为 0.8 μM。[1-4] |
| In Vitro | A-769662在激活杆状病毒表达的AMPK的α1，β1，γ1重组同种型(EC50 =0.7μM)方面同样有效。 A-769662和A-592107以剂量响应方式激活从多种组织和物种中纯化的AMPK，观察到的EC50具有适度的变化。使用来自大鼠心脏，大鼠肌肉或人胚肾细胞(HEK)的部分纯化的AMPK提取物测定的A-769662的EC50分别为2.2μM，1.9μM或1.1μM[1]。 A-769662激活表达LKB1(HEK293)和LKB1缺陷(CCL13)细胞中的内源AMPK。 A-769662变构激活含有γ1的AMPK复合物，其含有精氨酸残基298取代成甘氨酸(R298G)。 A-769662抑制含突变体γ1的复合物中Thr-172的去磷酸化程度与野生型复合物中所见的程度相似[2]。 A769662(300μM)对MEF细胞有毒性作用。 A769662可逆地抑制蛋白酶体活性[3]。 |
| In Vivo | A-769662(30mg / kg，ip)显著降低SD大鼠的呼吸交换率(RER)。用30mg / kg A-769662(0.905nmol / g)或500mg / kg二甲双胍(0.574nmol / g)处理的动物的肝脏中丙二酰辅酶A水平分别降低33％和58％。 A-769662(30 mg / kg，bid)显著降低了喂养血浆葡萄糖(降低30％-40％)，而较低剂量(3和10 mg / kg)的A-769662对糖尿病患者没有影响。 ob小鼠[1]。 |
| Animal Experiment | 适应后，将ob / ob和瘦小鼠随机分为各种治疗组，体重和喂食葡萄糖水平(尾部剪断)于上午8点。基线血浆胰岛素样品也取自代表每个治疗组的动物子集(n = 10 ob / ob和n = 10瘦ob / +同窝小鼠)。完成两个单独的ob / ob和瘦的同窝相研究：1)最初的5天研究，和2)14天研究以检查功效并且更完全地表征在5天研究中观察到的体重变化。 5天研究的治疗组如下：ob / ob载体(0.2％羟丙基甲基纤维素[HPMC]，ip，bid)，A-592107(10或100mg / kg，ip，bid)，A-769662(3)或30 mg / kg，ip，bid)，AICAR(375 mg / kg，sc，bid)，或二甲双胍(450 mg / kg，po，qd，含有载体的PM)，以及用载体治疗的瘦性同窝仔(ip，出价)。用于14天ob / ob和瘦同窝物研究的治疗组如下：ob / ob载体(0.2％HPMC，ip，bid)，A-769662(3，10或30mg / kg，ip，bid)，或二甲双胍，以及用载体或30mg / kg A-769662(ip，bid)治疗的瘦性同窝小鼠。 |
| Kinase Experiment | 为了测定糖原磷酸化酶b(GPb)活性，将1.5μg/ mL兔GPb加入到含有20mM Na 2 HPO 4(pH 7.2)，2mM MgSO4，1mMβ-NADP(β-烟酰胺腺嘌呤二核苷酸磷酸)的反应混合物中，1.4U / mL G-6-PDH(葡萄糖-6-磷酸 - 脱氢酶)和3U / mL PGM(磷酸葡糖苷酶)。将AMP或测试化合物以指定浓度加入测定培养基中，然后加入糖原(终浓度1mg / mL)以引发反应。在25℃温育10分钟后，通过测量340nm处的吸光度来评估GPb活性。 |
| Data Literature Source | [1]. Cool B，et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab，2006，3(6)，403-416. [2]. Sanders MJ，et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662，a member of the thienopyridone family. J Biol Chem，2007，282(45)，32539-32548. [3]. Moreno D，et al，A769662，a novel activator of AMP-activated protein kinase，inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett，2008，583(17)，2650-2654. [4]. Yerra VG，et al. Adenosine Monophosphate-Activated Protein Kinase Abates Hyperglycaemia-Induced Neuronal Injury in Experimental Models of Diabetic Neuropathy: Effects on Mitochondrial Biogenesis，Autophagy and Neuroinflammation. Mol Neurobiol. 2017 Apr;54(3):2301-2312. |
| Unit | Bottle |
| Specification | 2mg 5mg |
是一种有效的，可逆的AMPK激活剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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