生物活性 | |||
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描述 | LG-100064 is synthetic retinoid (3-methyl-TTNCB) working as a selective pan-RXR agonist with EC50 values of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ, with no activity on RARs. It has affinity to RXRα, RXRβ and RXRγ with Kd values of 350nM, 230nM and 365nM. LG-100064 is capable of inhibiting transglutaminase enzymatic activity with IC50 value of 0.1μM. A 0.1% solution of LG-100064 is capable of inhibiting the utriculi diameter by approximately 50% in Rhino mice topically dosed of LG-100064, with less irritating to the skin of Rhino mice than 9-cis- or all-trans-retinoic acid. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.85mL 0.57mL 0.29mL |
14.27mL 2.85mL 1.43mL |
28.53mL 5.71mL 2.85mL |