AGN 193109

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AGN 193109 是一种类维生素A类似物，是一种有效且特异性的 RAR 拮抗剂（RARα、RARβ 和 RARγ 的 Kds：2 nM、2 nM 和 3 nM）。AGN 193109 完全具有 RAR 特异性，因为它不结合或反式激活通过任何 RXR。

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).AGN 193109 is completely RAR specific because it does not bind to or transactivate through any of the RXRs . AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increases in levels of K7, K8, and K19 .AGN 193109 (0.30 or 1.20 μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment. AGN 193109 (1.15 μmol/kg) does not cause overt toxicity and has no effect on spleen weight on the mice, but it suppresses TTNPB-induced increase in spleen weight of the mice. AGN 193109 also significantly reduces the cutaneous toxicity induced by ATRA.(In Vitro):AGN 193109 (0.1 and 1 μmol/L; 3 w) dose-dependently increases vascular smooth muscle cells (VSMCs) mineralization.AGN 193109 (100?nM; 10 d) induces human pluripotent stem cells (hPSCs) differentiate into olfactory placode cells and neurons.

AGN 193109 (0.1 and 1 μmol/L; 3 w) dose-dependently increases vascular smooth muscle cells (VSMCs) mineralization.AGN 193109 (100?nM; 10 d) induces human pluripotent stem cells (hPSCs) differentiate into olfactory placode cells and neurons.

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Metabolic Enzyme/Protease

Retinoid Receptor

RARα| RARβ| RARγ

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171746-21-7

392.49

C28H24O2

>98% (HPLC)

DMSO:2 mg/mL (5.10 mM; Need warming)

Cc1ccc(cc1)C1=CCC(C)(C)c2ccc(cc12)C#Cc1ccc(cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years