CAS:94497-51-5
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
Tamibarotene是视黄酸受体α/β (RARα/β)的激动剂。
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TamibaroteneCAS:94497-51-5
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
CAS | 94497-51-5 |
Chinese Name | 他米巴罗汀 |
English Name | Tamibarotene |
Synonyms | Am 80;Amnolake;NSC 608000 |
Molecular Formula | C22H25NO3 |
Molecular Weight | 351.44 |
Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
Purity | ≥98% |
Appearance | White to yellow Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 1806241-263-5 |
MDL | MFCD00866188 |
SMILES | O=C(C1=CC=C(C=C1)C(NC2=CC=C3C(C)(CCC(C)(C3=C2)C)C)=O)O |
Target Point | RAR(RARα,RARβ) |
Passage | Metabolic Enzyme&Protease |
Background | Tamibarotene is a retinoic acid receptor alpha/beta (RARalpha/beta) agonist. |
Biological Activity | Tamibarotene是视黄酸受体α/β (RARα/β)的激动剂,比RARγ的选择性高。[1-5] |
In Vitro | 他米巴罗汀(20,40μM)下调T细胞淋巴瘤细胞中细胞周期基因的表达。他米巴罗汀(5μM)使RARA过表达细胞中的RARE活性增加到比RARAlow细胞更大的程度。此外,RARAwt过表达增加了他米巴罗汀治疗引起的CDK2,CDK4和CDK6抑制的程度[1]。他米巴罗汀直接逆转转化生长因子-β1处理的真皮成纤维细胞的促纤维化表型,抑制内皮细胞中ICAM-1的表达,并促进体外M1巨噬细胞分化[2]。他米巴罗汀(4μM)在VSMC中剂量依赖性地上调apelin mRNA和蛋白质水平。在Tamibarotene刺激后,RARα(视黄酸受体α)通过与KLF5和Sp1相互作用而募集到apelin启动子,预先与apelin启动子的TCE位点结合,形成转录激活复合物,随后导致apelin表达的上调。在VSMC中。 KLF5和Sp1通过它们与apelin启动子上的TCE直接结合,共同介导他米巴罗汀诱导的apelin表达[4]。 |
In Vivo | 他米巴罗汀(1mg / kg /天)分别显着减弱博来霉素(BLM)处理的小鼠和紧致皮肤1小鼠的皮肤和皮下纤维化。一致地,他米巴罗汀显着抑制与组织纤维化相关的各种分子的表达,包括转化生长因子-β1,结缔组织生长因子,IL-4,IL-10,IL-13,IL-17A,肿瘤坏死因子-α,IFN -γ和BLM处理小鼠的损伤皮肤中的单核细胞趋化蛋白1。此外,Tamibarotene降低效应T细胞的比例,同时增加BLM处理小鼠引流淋巴结中CD4 + T细胞中幼稚T细胞的比例[2]。与未治疗的小鼠相比,他米巴罗汀(2.5mg / kg,口服)不会导致牙周炎攻击小鼠的AST,ALT或ALP血清水平的任何显着改变。他米巴罗通改善牙槽骨吸收,显着减少小鼠牙龈卟啉单胞菌诱导的破骨细胞数量。与EPD小鼠相比,他米巴罗汀可测量地增加CD4 + Foxp3 + Treg细胞的百分比。他米巴罗汀还有效降低牙龈卟啉单胞菌感染的牙龈组织和CLN中CD4 + ROR-γt+(Th17)细胞的表达[3]。他米巴罗汀(1 mg / kg,po)可增加大鼠球囊损伤动脉的apelin表达,与培养的VSMCs结果一致[4]。在老年SAMP8小鼠中,在施用他米巴罗汀(1mg / kg /天)后海马ADAM10水平改善。在Tamibarotene给药后,Hes5和Ki67恢复,空间工作记忆也得到改善[5]。 |
Cell Experiment | CellTiter水性非放射性细胞增殖测定试剂盒用于评估细胞生长。简言之,将每孔10,000个细胞接种在96孔板中,并在含有2%活性炭剥离的FBS的RPMI中培养,并指示类视黄醇浓度72小时。在处理期结束时,加入MTS试剂,将细胞再孵育2-4小时,并在490纳米下测量吸光度。 |
Animal Experiment | 对于感染,给小鼠口服悬浮液中的磺胺甲恶唑和甲氧苄氨嘧啶10mL去离子水10天,以减少天然菌群并支持牙龈卟啉单胞菌W83的定植。抗生素治疗结束后4天,通过口服接种建立牙周感染,使用悬浮在100μL4%羧甲基纤维素(CMC)中的1010菌落形成单位的牙龈卟啉单胞菌7天。在第一次口服接种后4周对小鼠实施安乐死。将他米巴罗汀(2.5mg / kg)悬浮在0.5%羧甲基纤维素溶液中。每天以0.1mL / 10g体重的体积将药物口服加入食道。在诱导牙周炎之前1小时施用他米巴罗汀,然后按照方案每天给予直至第28天。患有牙周病的对照小鼠接受相同体积的0.5%羧甲基纤维素溶液。每3天测量每只小鼠的体重。 |
Data Literature Source | [1]. Wang X,et al. Retinoic acid receptor alpha drives cell cycle progression and is associated with increased sensitivity to retinoids in T-cell lymphoma. Oncotarget. 2017 Apr 18;8(16):26245-26255. [2]. Toyama T,et al. Tamibarotene Ameliorates Bleomycin-Induced Dermal Fibrosis by Modulating Phenotypes of Fibroblasts,Endothelial Cells,and Immune Cells. J Invest Dermatol. 2016 Feb;136(2):387-98. [3]. Jin Y,et al. Tamibarotene modulates the local immune response in experimental periodontitis. Int Immunopharmacol. 2014 Dec;23(2):537-45. [4]. Lv XR,et al. Synthetic retinoid Am80 up-regulates apelin expression by promoting interaction of RARα with KLF5 and Sp1 in vascular smooth muscle cells. Biochem J. 2013 Nov 15;456(1):35-46. [5]. Kitaoka K,et al. The retinoic acid receptor agonist Am80 increases hippocampal ADAM10 in aged SAMP8 mice. Neuropharmacology. 2013 Sep;72:58-65 |
Unit | Bottle |
Specification | 10mg 25mg |
Tamibarotene是视黄酸受体α/β (RARα/β)的激动剂。