AM580
货号:A184890 同义名:
CD336;Ro 40-6055
AM580 是一种稳定的视黄酸苯甲酸衍生物,作为 RARα 的激动剂。
AM580 化学结构 CAS号:102121-60-8 AM580 3D分子结构 CAS号:102121-60-8 规格 价格 库存 数量 100μL*10mM(DMSO) ¥109 咨询 250μL*10mM(DMSO) ¥229 咨询 500μL*10mM(DMSO) ¥299 咨询 10mM*1mL(DMSO) ¥462 咨询 1mg ¥171 咨询 5mg ¥378 咨询 10mg ¥567 咨询 25mg ¥1276 咨询 50mg ¥2169 咨询 100mg ¥3458 咨询
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更多 > AM580 质控信息
AM580 生物活性 描述 AM580 is a retinoic acid analog, working as a selective RARα agonist with EC50 values of 0.3, 8.6 and 13 nM for RARα, RARβ and RARγ respectively. AM580 at concentration of 100nM could recapitulate all of the T cell activation and type 2 cytokine-inducing effects of ATRA and 9-cis-RA on promotion of IL-4, IL-5 and IL-13 synthesis, while decreasing IFN-γ and TNF-α expression by activated human T cells and reduces the synthesis of IL-12p70 from accessory cells. Enhancing RA signaling by AM580 at concentration of 10nM profoundly promoted reprogramming of MEFs with transfected with four transcription factors (Oct4, Sox2, c-Myc, and Klf4), shown as substantial increase of the number of AP+ iPSC colonies.
AM580 动物研究 Dose Mice: 3.75 mg/kg[3] (i.p.), 2 mg/kg - 10 mg/kg[4] (i.p.), 12.5 mg/kg (i.p.); 0.3 mg/kg[1] (p.o., in diet), 0.6 mg/kg - 0.8 mg/kg[5] (p.o., in drinking water) Administration i.p., p.o. Pharmacokinetics
Animal
Rats[4]
Dose
10 mg/kg
Administration
i.p.
Vd 1.5 ± 0.7 L/kg
T1/2 1.7 ± 0.3 h
Tmax 0.6 ± 0.4 h
CL
9.7 ± 3.2 ml/min/kg
Cmax 5.8 ± 2.1 μg/ml
AUC
18.4 ± 5.4 μg·h/ml
AM580 参考文献 [1] Lu Y, Bertran S, et al. Mechanism of inhibition of MMTV-neu and MMTV-wnt1 induced mammary oncogenesis by RARalpha agonist AM580. Oncogene. 2010 Jun 24;29(25):3665-76.
[2] Gianni M, Li Calzi M, et al. AM580, a stable benzoic derivative of retinoic acid, has powerful and selective cyto-differentiating effects on acute promyelocytic leukemia cells. Blood. 1996 Feb 15;87(4):1520-31.
[3] Nishikiori N, Osanai M, et al. Inhibitory effects of retinoic acid receptor alpha stimulants on murine cataractogenesis through suppression of deregulated calpains. Invest Ophthalmol Vis Sci. 2007 May;48(5):2224-9.
[4] Dimitrova B, Caccia S, et al. Determination of the retinobenzoic acid derivative Am580 in rat plasma by high-performance liquid chromatography. J Chromatogr B Biomed Appl. 1995 May 19;667(2):301-6.
[5] Melis M, Tang XH, et al. Effects of AM80 compared to AC261066 in a high fat diet mouse model of liver disease. PLoS One. 2019 Jan 24;14(1):e0211071.
展开 AM580 实验方案 计算器 摩尔计算器 总药量计算器 工作液计算器 存储液制备 1mg 5mg 10mg 1 mM
5 mM
10 mM
2.85mL
0.57mL
0.28mL
14.23mL
2.85mL
1.42mL
28.45mL
5.69mL
2.85mL
AM580 技术信息