ETC-1002
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ETC-1002是一种可口服的ACL抑制剂(IC50= 29 μM)和AMPK激活剂。
在体外,ETC-1002可提高AMP活化的蛋白激酶(AMPK)磷酸化水平,降低MAP激酶活性,并能减少促炎细胞因子和趋化因子的合成。这些对炎症可溶性介质的效果可被LKB1 siRNA显著抵消,表明ETC-1002可活化AMPK,并通过LKB1依赖的机制发挥其抗炎活性[1]。
在体内, ETC-1002可抑制巯基乙酸诱导的淋巴细胞流入小鼠腹腔。在饮食诱发肥胖的小鼠模型中,ETC-1002可恢复脂肪AMPK活性,降低JNK磷酸化,并能减弱巨噬细胞特异标记物4F/80的表达。[1]
在临床试验中,ETC-1002可降低低密度脂蛋白-胆固醇(LDL-C)和其他脂类,并能提高2型糖尿病和高胆固醇血症病人中高敏感性C反应蛋白,而不至于恶化血糖控制。ETC-1002在这些人群中有低毒性。[2]
参考文献:
1. Filippov S1, Pinkosky SL, Lister RJ et al. ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK. J Lipid Res. 2013 Aug;54(8):2095-108.
2. Gutierrez MJ1, Rosenberg NL, Macdougall DE et al. Efficacy and safety of ETC-1002, a novel investigational low-density lipoprotein-cholesterol-lowering therapy for the treatment of patients with hypercholesterolemia and type 2 diabetes mellitus. Arterioscler Thromb Vasc Biol. 2014 Mar;34(3):676-83.
Storage | Store at -20°C |
M.Wt | 344.49 |
Cas No. | 738606-46-7 |
Formula | C19H36O5 |
Solubility | insoluble in H2O; ≥97.6 mg/mL in DMSO; ≥42.5 mg/mL in EtOH |
Chemical Name | 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid |
SDF | Download SDF |
Canonical SMILES | OC(C(C)(C)CCCCCC(O)CCCCCC(C)(C)C(O)=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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