RXR antagonist 1

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RXR antagonist 1 

RXR antagonist 1 (compound 6a) 是一种类视黄醇 X 受体 (Retinoid X Receptor (RXR)) 调节剂。RXR antagonist 1 具有较强的 RXR 拮抗活性，其 pA2 为 8.06。RXR antagonist 1 可用于 2 型糖尿病的研究。

RXR antagonist 1

RXR antagonist 1 Chemical Structure

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生物活性

RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research[1].

IC50 & Target

RXR

8.06 (pA2)

体外研究
(In Vitro)

RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM[1].
RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39[1].
The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.57

Formula

C28H33F3N2O3
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.
参考文献

  • [1]. Masaki Watanabe, et al. Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators. ACS Med. Chem. Lett. 2022, 13, 2, 211-217.

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