ABT-046
目录号: PL14718 纯度: ≥98%
CAS No. :1031336-60-3
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中文名称
ABT-046
中文别名
反式-4-[4-(7-氨基吡唑并[1,5-A]嘧啶-6-基)苯基]环己烷乙酸
英文名称
ABT-046
英文别名
2-(trans-4-(4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl)cyclohexyl)acetic acid;ABT-046;2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid;ABT 046;AK143027;CHEMBL2165819;CS-1213;DGAT-1 inhibitor;HY-15197;SureCN4943142;trans {4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl}acetic acid;trans-{4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl}acetic acid;trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid;2-((1R,4R)-4-(4-(7-AMINOPYRAZOLO[1,5-A]PYRIMIDIN-6-YL)PHENYL)CYCLOHEXYL)ACETIC ACID;Cyclohexaneacetic acid, 4-[4-(7-aMinopyrazolo[1,5-a]pyriMidin-6-yl)phenyl]-, trans-
Cas No.
1031336-60-3
分子式
C20H22N4O2
分子量
350.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ABT-046 是一种具有口服活性的选择性二酰基甘油酰基转移酶 1 (DGAT-1) 抑制剂,对人和小鼠 DGAT-1 的 IC50 均为 8 nM。
生物活性
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC 50 s of both 8 nM against human and mouse DGAT-1.
性状
Solid
IC50 & Target[1][2]
IC50: 8 nM (hDGAT-1 and mDGAT-1)
体外研究(In Vitro)
ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 of 78 nM.
ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively).
ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice.
ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yeh VS, et al. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of Acyl-CoA: Diacylglycerol acyltransferase 1. J Med Chem. 2012 Feb 23;55(4):1751-1757.
溶解度数据
In Vitro: DMSO : 66.67 mg/mL (190.26 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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