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Tamibarotene

  • 產品貨號：CS-01Y66109
  • 產品價格：電議
  • 產品產地：進口、國產
  • 包裝類型:10mM (in 1mL DMSO) 10mg 50mg
  • 采購熱度：232
  • 庫存：100
  • CAS號：94497-51-5
  • 方法：
  • 含量：>98.00%
  • 品牌名稱:莼試
  • 分子式：C22H25NO3
  • 分子量：351.44

簡介內容：質量保證、價格優惠

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產品目錄

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 化學性質：                                                                                                             

規格

10mM (in 1mL DMSO) 10mg 50mg

CAS

94497-51-5

別名

Am80;Am 80;Am-80

化學名

4-[(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)carbamoyl]benzoic acid

分子式

C22H25NO3

分子量

351.44

溶解度

≥ 13.35 mg/mL in DMSO, ≥ 52.5 mg/mL in EtOH with ultrasonic

儲存條件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

產品描述：                                                                                                             

Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.

Tamibarotene (20, 40 μM) down-regulates expression of cell cycle gene in T-cell lymphoma cells. Tamibarotene (5 μM) increases RARE activity in RARA-overexpressing cells to a much greater degree than in RARAlow cells. Moreover, RARAwt overexpression augments the degree of CDK2, CDK4, and CDK6 inhibition caused by Tamibarotene treatment[1]. Tamibarotene directly reverses the profibrotic phenotype of transforming growth factor-β1-treated dermal fibroblasts, suppresses ICAM-1 expression in endothelial cells, and promots M1 macrophage differentiation in vitro[2]. Tamibarotene (4 μM) up-regulates apelin mRNA and protein levels dose-dependently in VSMCs. Upon Tamibarotene stimulation, the RARα (retinoic acid receptor α) is recruited to the apelin promoter by interacting with KLF5 and Sp1 prebound to the TCE site of the apelin promoter to form a transcriptional activation complex, subsequently leading to the up-regulation of apelin expression in VSMCs. KLF5 and Sp1 co-operatively mediate Tamibarotene-induced apelin expression through their direct binding to the TCE on the apelin promoter[4].

Tamibarotene (1 mg/kg/day) significantly attenuates dermal and hypodermal fibrosis in bleomycin (BLM)-treated mice and tight skin 1 mice, respectively. Consistently, Tamibarotene significantly suppresses the expression of various molecules related to tissue fibrosis, including transforming growth factor-β1, connective tissue growth factor, IL-4, IL-10, IL-13, IL-17A, tumor necrosis factor-α, IFN-γ, and monocyte chemotactic protein 1 in the lesional skin of BLM-treated mice. Furthermore, Tamibarotene decreases the proportion of effector T cells, while increasing that of naive T cells among CD4+ T cells in the draining lymph nodes of BLM-treated mice[2]. Tamibarotene (2.5 mg/kg, p.o.) does not result in any significant alteration of the AST, ALT, or ALP serum levels in periodontitis-challenged mice compared with that in untreated mice. Tamibarotene ameliorates alveolar bone resorption, significantly reduces the number of P. gingivalis-induced osteoclasts in mice. Tamibarotene measurably increases the percentage of CD4+ Foxp3+ Treg cells as compared to those in EPD mice. Tamibarotene is also effective in reducing the expression of CD4+ROR-γt+ (Th17) cells in P. gingivalis-infected gingival tissues and CLNs[3]. Tamibarotene (1 mg/kg, p.o.) increases apelin expression in balloon-injured arteries of rats, consistent with the results from the cultured VSMCs[4]. In aged SAMP8 mice, hippocampal ADAM10 levels improve after Tamibarotene (1 mg/kg/day) administration. Hes5 and Ki67 are restored and spatial working memory also improves after Tamibarotene administration[5].

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1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創作者：上海莼試生物技術有限公司

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