LG100268 (Synonyms: LG268)
目录号: PL10807 纯度: ≥98%
CAS No. :153559-76-3
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中文名称
LG100268
中文别名
6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸;6-[1-(5,6,7,8-四氢-3,5,5,8,8-戊甲基-2-萘基)氯丙基]-3-吡啶羧酸
英文名称
LG100268
英文别名
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID;3-Pyridinecarboxylicacid,6-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)cyclopropyl]-;6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid;6-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)cyclopropyl]-3-Pyridinecarboxylic Acid;LG 100268;6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRO-NAPHTHALEN-2-YL)-CYCLOPROPYL]-NICOTINIC ACID (FOR R&AmbkkkkK580;BIDD:PXR0022;2-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)cyclopropyl]pyridine-5-carboxylic acid;AGN 192620;ALRT 268.;CD 3127;LG268;LGD 100268;LGD 1268;ALRT 268;LG 268;lg100268;hthalenyl)cyclopropyl)-;3-pyridinecarboxylicacid,6-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-nap;LG100268
Cas No.
153559-76-3
分子式
C24H29NO2
分子量
363.49
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
LG100268 (LG268) 是一种有效的、选择性的,具有口服活性的视黄素X受体 (RXR) 激动剂,对 RXR-α,RXR-β,和RXR-γ 的 EC50 值分别为 4 nM、3 nM、4 nM。LG100268 显示对 RXR 的选择性优于 RAR (1000 倍), 对 RXR-α,RXR-β,和 RXR-γ 的 Ki 值分别为 3.4 nM,6.2 nM 和 9.2 nM。LG100268 激活 RXR 同源二聚体,诱导转录激活。LG100268 可用于肺癌的研究。
生物活性
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC 50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the K i values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
性状
Solid
体外研究(In Vitro)
LG100268 (100 nM-1 μM; 24 hours) shows a downregulation of CSF3 and a 2.5-fold decrease of CXCL2 and IL-1β mRNA expression in RAW264.7 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) combines with C/P presents a more markedly reduced average tumor burden than LG268 or C/P alone. The combination establish a reduced lung tumors, which represents a reduction of 82% (vs. 59%-67% with the single drugs) in comparison with the controls.
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]. M F Boehm, et al. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem
[2]. D S Lala, et al. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383(6599):450-3.
[3]. Martine Cao,et al.The Rexinoids LG1
溶解度数据
In Vitro: DMSO : 5.56 mg/mL (15.30 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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