CAS: 67-30-1; Tetrac

该化合物是甲状腺素(T4)的合成衍生物,其特点是其芳香结构中含有四碘原子,众所周知,该化合物在影响代谢过程方面起着作用,并已研究其潜在的治疗用途,特别是在甲状腺激素管制方面;四碘代新酸因其含碘含量而表现出高脂性,从而影响其溶解性和生物利用率;通常以晶体形式出现,在标准实验室条件下保持稳定;该化合物与甲状腺激素受体发生相互作用,影响基因表达和代谢途径;其药理特性使其成为内分泌学和代谢研究的一个主题;然而,与许多含碘化合物一样,告诫应谨慎使用该物质,因为过度的碘可导致甲状腺功能失调.

结构式图片

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CAS号1155-40-4 3,5-二碘-THYRO乙酸 | CAS号83799-60-4 (4-hydroxy-3,5-... | CAS号861065-72-7 [4-(4-methoxy-p... | CAS号150-76-5 4-甲氧基苯酚(MEHQ) | CAS号85828-82-6 ethyl 3,5-diiod... | CAS号101588-11-8 ethyl 2-(3,5-di... | CAS号860687-73-6 1-(4-chlorometh... | CAS号855937-68-7 [3,5-diiodo-4-(...

合成工艺路线路线简述

    Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于水体系中,化学反应生成 3,3,5,5-四碘甲腺乙酸
    参考文献:Pitt-Rivers; James,Biochemical Journal,1958,Vol. 70,P. 173,174
    标题:Pitt-Rivers; James,Biochemical Journal,1958,Vol. 70,P. 173,174

    海关参考信息

    专利信息


    专利号:US-10413555-B2
    优先权日:2014-11-25
    标题:Treatment of skin atrophy with a combination of triiodothyroacetic acid (TRIAC) and dehydroepiandrosterone (DHEA)
    发明人:FAERGEMANN JAN; JOHANNSSON GUDMUNDUR; OHLSSON CLAES; BATCHELLER DEREK GREGORY; JOHNSSON JÖRGEN; TÖRNELL JAN
    权利人:TROPHEA DEV AB
    摘要:The aim of the present study was to investigate the effect of a combination of triiodothyroacetic acid (TRIAC) and dehydroepiandrosterone (DHEA) compared with TRIAC, DHEA or placebo alone on corticosteroid induced effect on collagen synthesis in humans. Six healthy male human volunteers aged 40-65 participated. Four areas of abdominal skin were pre-treated for 3 weeks with betamethasone valerate cream. The same areas were then treated with one of the following alternatives in the same cream vehicle: TRIAC, DHEA, TRIAC+DHEA and placebo for 2 weeks. Then suction blisters were raised in each of these areas with a vacuum pump. The blister fluid from each area was collected and frozen until analysis. Analysis of amino terminal propeptide of human type I procollagen (PINP) in suction blister fluid was performed using a commercially available immunoassay (Orion Diagnostics) kit. This study has for the first time shown that a combination of TRIAC and DHEA could effectively stimulate collagen synthesis in skin pretreated with betamethasone valerate demonstrated by an increase in PINP, and that the combination was more effective than TRIAC or DHEA alone. This combination could be used to effectively treat skin atrophy in corticosteroid induced skin atrophy. It could also be used to treat skin atrophy due to other circumstances such as e. g. sun damaged skin and skin atrophy due to high age. Another interesting application would be to combine TRIAC and DHEA with a potent corticosteroid in order to prevent corticosteroid induced skin atrophy. If this combination still is effective in the treatment of eczema and psoriasis and without the risk of skin atrophy this combination will be a major breakthrough for the use of potent topical corticosteroids.

    专利号:US-11186551-B2
    优先权日:2020-04-29
    标题 :Composition of scalable thyrointegrin antagonists with improved retention in tumors
    发明人:MOUSA SHAKER A; HAY BRUCE A
    权利人:NANOPHARMACEUTICALS LLC
    摘要:Chemical compounds/compositions, methods of synthesis, and methods of use. The compounds/compositions are directed toward thyrointegrin antagonists conjugated to a polymer. The compounds/compositions further comprise an additional substituent also conjugated to the polymer. The compounds/compositions demonstrate increased uptake across the blood brain barrier along with increased retention therein and retention within tumor. The compounds/compositions may also include improved synthesis scalability, improved purity, improved aqueous solubility, and a solid product or intermediate. The compounds/compositions may demonstrate improved antiangiogenic effect and improved efficacy against conditions, particularly cancers, requiring blood brain barrier permeability, for example, glioblastoma (GBM).

    专利号:WO-2022260918-A1
    优先权日:2021-06-07
    标 题:Composition and method for dual targeting in treatment of neuroendocrine tumors
    发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O
    权利人:NANOPHARMACEUTICALS LLC
    摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone ανβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.

    专利号:US-11077082-B2
    优先权日:2018-04-11
    标题 :Composition and method for dual targeting in treatment of neuroendocrine tumors
    发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O
    权利人:NANOPHARMACEUTICALS LLC
    摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone αvβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.

    专利号:JP-2021505618-A
    优先权日:2017-12-06
    标题:Solid-phase synthesis of NIR fluorescent probe

    专利号:US-11351137-B2
    优先权日:2018-04-11
    标题 :Composition and method for dual targeting in treatment of neuroendocrine tumors
    发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O
    权利人:NANOPHARMACEUTICALS LLC
    摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone αvβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.
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    主要参考文献

    [参考文献]: Ashur-Fabian O, Et, Al. Tetrac Delayed The Onset Of Ocular Melanoma In An Orthotopic Mouse Model. Front Endocrinol (Lausanne). 2019 Jan 8; 9:775.
    [参考文献]: Chin Yt, Et, Al. Tetrac And Ndat Induce Anti-Proliferation Via Integrin αvβ3 In Colorectal Cancers With Different K-Ras Status. Front Endocrinol (Lausanne). 2019 Mar 12; 10:130.
    [参考文献]: Davis Pj, Et, Al. Nongenomic Actions Of Thyroid Hormone: The Integrin Component. Physiol Rev. 2020 Jun 25.
    [参考文献]: Rajabi M, Et, Al. Synthesis Of New Analogs Of Tetraiodothyroacetic Acid (Tetrac) As Novel Angiogenesis Inhibitors For Treatment Of Cancer. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1223-1227.
    [参考文献]: Schmohl Ka, Et, Al. Tetrac As An Anti-Angiogenic Agent In Cancer. Endocr Relat Cancer. 2019 Jun 1; 26(6):R287-R304.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    参考文献:10.1210/endo-107-1-176
    摘要:Takai NA, Rapoport B, Yamamoto M. Biliary excretion of iodothyronines in rats as determined by high pressure liquid chromatography: effect of starvation. Endocrinology. 1980 Jul;107(1):176–82. doi: 10.1210/endo-107-1-176.
    参考文献:10.1016/j.ijpharm.2008.04.018
    摘要:Shah RB, Bryant A, Collier J, Habib MJ, Khan MA. Stability indicating validated HPLC method for quantification of levothyroxine with eight degradation peaks in the presence of excipients. International Journal of Pharmaceutics. 2008 Aug;360(1-2):77–82. doi: 10.1016/j.ijpharm.2008.04.018.
    参考文献:10.1210/jc.2009-1926
    摘要:Yalcin M, Dyskin E, Lansing L, Bharali DJ, Mousa SS, Bridoux A, Hercbergs AH, Lin HY, Davis FB, Glinsky GV, Glinskii A, Ma J, Davis PJ, Mousa SA. Tetraiodothyroacetic acid (tetrac) and nanoparticulate tetrac arrest growth of medullary carcinoma of the thyroid. J Clin Endocrinol Metab. 2010 Apr;95(4):1972–80. doi: 10.1210/jc.2009-1926.
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