2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. LG101506

LG101506 是一种选择性和口服活性的 RXR 调节剂，对 RXRα 的 Ki 为 2.7 nM。LG101506 可用于研究 2 型糖尿病和癌症。

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LG101506 Chemical Structure

LG101506 Chemical Structure

CAS No. : 331248-11-4

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LG101506 相关抗体

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查看 RAR/RXR 亚型特异性产品:

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RXRα RXRβ RXRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer[1][2].

IC50 & Target

Ki: 2.7 nM (RXRα)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CV-1 EC50
131.5 nM
Compound: 4
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
[PMID: 12954061]
体外研究
(In Vitro)

LG101506 与 BRL 49653 (HY-17386) 协同作用增强 RXR/PPARγ 异源二聚体的激活，EC50 为 3.1 nM[1]。
LG101506 (15.6-1000 nM) 以剂量依赖的方式阻断 LPS (HY-D1056) 刺激 RAW264.7 细胞 24 小时内 NO 的产生[2]。
LG101506 (100-1000 nM; 24 h) 在 RAW264.7 细胞中抑制 LPS (HY-D1056) 或 TNFα 诱导的炎症通路[2]。
LG101506 (30 and 100 nM; 1-24 h) 诱导 U937 白血病细胞分化[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LG101506 相关抗体:

Western Blot Analysis[2]

Cell Line: RAW264.7 cells
Concentration: 100, 300 and 1000 nM
Incubation Time: 24 h
Result: Markedly reduced protein levels of COX-2. Pretreatment prevented the degradation of IκBα in RAW cells stimulated with TNFα. Enhanced Erk phosphorylation, which peaked at 8 hours.

Western Blot Analysis[2]

Cell Line: U937 leukemia cells
Concentration: 30 and 100 nM
Incubation Time: 1, 2, 8 and 24 h
Result: Enhanced phosphorylation of Akt in U937 cells within 1 hour, which increased further at 8 hours.
体内研究
(In Vivo)

LG101506 (10 mg/kg; in diet for 16 weeks) 抑制 A/J 小鼠肺癌的发生[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A/J mice, lung carcinogenesis model[2]
Dosage: 40 mg/kg diet or approximately 10 mg/kg body weight
Administration: Oral, for 16 weeks
Result: Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
Animal Model: Male ICR mice[1]
Dosage: 30 mg/kg
Administration: Oral (Pharmacokinetic Analysis)
Result: In vivo evaluation of oral exposure of LG101506[1]
Compd Dose (mg/kg) Oral AUC(0-6 h) (μg•h/mL) Tmax (h) Cmax (μg•h/mL)
LG101506 30 2.09±0.45 1 1.2±0.28

Data collected in male ICR mouse using a dose formulation of the free acid in CMC/SLS/Povidone (30 mg/kg). Timepoints: 1, 3, 8 h (serial sacrifice, n=3/time point).
分子量

420.53

Formula

C25H34F2O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LG101506 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LG101506331248-11-4LG 101506LG-101506RAR/RXRRetinoic acid receptorsRetinoid X receptorsanti-inflammatorycancertype 2 diabetesRAW264.7TNFαInhibitorinhibitorinhibit

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目录号：
HY-108524
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