2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. AGN-191659

AGN-191659 是一种具有口服活性的 RAR/RXR 激动剂，对 RXRα、RARβ、RARγ 的 EC50 值分别为 11 nM、23 nM、37 nM。AGN-191659 可激活 RXRα、RARβ 和 RARγ 以诱导基因转录。AGN-191659 可诱导组织型转谷氨酰胺酶活性，抑制促肿瘤剂诱导的鸟氨酸脱羧酶活性，抑制软骨形成。AGN-191659 逆转碱性成纤维细胞生长因子诱导的内皮细胞增殖。AGN-191659 在大鼠模型中诱导高甘油三酯血症。AGN-191659 抑制总肝素可释放脂肪酶活性。AGN-191659 可用于早幼粒细胞白血病、高甘油三酯血症的相关研究。

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AGN-191659

AGN-191659 Chemical Structure

CAS No. : 156691-86-0

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AGN-191659 相关抗体

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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

AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia[1][2][3].

IC50 & Target[1]

RXR α

11 nM (EC50)

体外研究
(In Vitro)

AGN-191659 (Compound 6) 在表达嵌合视黄酸受体的 HeLa 细胞中作为泛激动剂，可激活 ER-RARβ (EC50 = 23 nM)、ER-RARγ (EC50 = 37 nM) 和 ER-RXRα (EC50 = 11 nM)[1]。
AGN-191659 (24 h) 可在人早幼粒白血病细胞 HL-60 cdm-1 中诱导组织型转谷氨酰胺酶活性，其 EC50 = 5 nM[1]。
AGN-191659 (72 h) 可抑制第 11 天小鼠胚胎肢芽细胞高密度微团培养中的软骨形成，其 IC50 为 15 nM[1]。
AGN-191659 可与 RXR α、RXR β、RXR γ 及 RAR β 结合，对应的 Kd 值分别为 120 nM、139 nM、214 nM 和 2700 nM[2]。
AGN-191659 (0.001-10 μM; 24 h) 可通过[3H]胸苷掺入实验抑制 bFGF 诱导的第 2-3 代犬主动脉内皮细胞增殖，其 IC50 为 50 nM[2]。
AGN-191659 (0.001-10 μM; 48 h) 可剂量依赖性地抑制生长停滞的犬主动脉内皮细胞中由 bFGF 诱导的细胞数量增加[2]。

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

AGN-191659 相关抗体:

Cell Proliferation Assay[2]

Cell Line: Passage 2-3 canine aortic endothelial cells
Concentration: 0.001-10 μM
Incubation Time: 24 h (total, co-incubated with 10 ng/mL bFGF)
Result: Inhibited bFGF-induced [3H]thymidine incorporation with an IC50 of 50 nM.
Reduced incorporation to near 10% of bFGF-stimulated control levels at 10 μM.

Cell Proliferation Assay[2]

Cell Line: Growth-arrested canine aortic endothelial cells
Concentration: 0.001-10 μM
Incubation Time: 48 h (co-incubated with 10 ng/mL bFGF)
Result: Dose-dependently reduced bFGF-induced increases in cell number.
Reduced cell number to ~5000 cells (from ~30,000 in bFGF-only controls) at 10 μM.
体内研究
(In Vivo)

AGN-191659 (局部给药；TPA 处理前 1 小时) 可抑制无毛小鼠皮肤中 TPA (HY-18739) 诱导的鸟氨酸脱羧酶 (ODC) 活性，其 IC80 为每只小鼠 5.4 nmol[1]。
AGN-191659 (10-250 μmol/kg；口服；每日；连续 3 天) 可剂量依赖性地在雄性 Fischer 大鼠中诱发严重高甘油三酯血症[3]。

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

Animal Model: CDF (F-344)/CrlBR (male, 6-7 weeks old)[3]
Dosage: 10 μmol/kg; 30 μmol/kg; 100 μmol/kg; 250 μmol/kg; 20 μmol/kg
Administration: p.o.; daily; 3 consecutive days
Result: Induced a 6-fold elevation in serum triglycerides (mean ~290 mg/dL, significantly different from vehicle control).
Induced an ~8-fold elevation in serum triglycerides (mean ~400 mg/dL, significantly different from vehicle control).
Induced an ~9-fold elevation in serum triglycerides (mean ~460 mg/dL, significantly different from vehicle control) with 13% weight loss in treated rats.
Induced an ~9-fold elevation in serum triglycerides (mean ~480 mg/dL, significantly different from vehicle control) with 23% weight loss in treated rats.
Reduced plasma post-heparin lipolytic activity by 89% (mean 4.7 nmol/min/mL, significantly different from vehicle control) and increased serum triglycerides to a mean of 589 mg/dL (significantly different from vehicle control).
分子量

368.54

Formula

C23H28O2S
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

AGN-191659 相关分类

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  • 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:

AGN-191659156691-86-0AGN191659AGN 191659RAR/RXRRetinoic acid receptorsRetinoid X receptorsRAR/RXR agonistpromyelocytic leukemiahypertriglyceridemiaCDF (F-344)/CrlBR ratInhibitorinhibitorinhibit

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