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3,3',5-三碘- l -甲状腺原氨酸(钠盐水合物)

TRα和TRβ激动剂

产品号 #(选择产品)

产品号 #100-0548_C

TRα和TRβ激动剂

总览

3,3',5-三碘- L-甲状腺原氨酸是一种甲状腺激素,它是通过脱碘作用由促甲状腺激素原转化而来的(Misiti et al.)。3,3',5-三碘- L-甲状腺原氨酸与甲状腺激素受体TRα和TRβ (Kd = 0.06 nM);Sandler et al.),并对多种细胞类型的生长和分化至关重要(Misit et al.;Shiohara et al.)。3,3',5-三碘- L-甲状腺原氨酸能抑制垂体细胞对亮氨酸的摄取(IC50 = 2 μM;Yan & Hinkle)。本品以水合钠盐形式供应。

分化
·促进人类多能干细胞分化为胰腺β细胞(Pagliuca et al.)。
癌症研究
·抑制胰腺腺癌的增殖(Michienzi et al.)。

别名
左旋甲状腺素,T3,L‑3,3′,5‑三碘甲腺原氨酸
 
细胞类型
胰腺细胞
 
应用
分化
 
研究领域
癌症
 
CAS 编号
345957-19-9
 
化学式
C15H11I3NO4 • Na • XH2O
 
分子量
673 克/摩尔
 
纯度
≥98%
 

Protocols and Documentation

Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.

Document Type
Product Name
Catalog #
Lot #
Language
Catalog #
100-0548, 100-0549
Lot #
All
Language
English
Document Type
Safety Data Sheet
Catalog #
100-0548, 100-0549
Lot #
All
Language
English

Resources and Publications

Educational Materials (5)

Publications (6)

Generation of functional human pancreatic $\beta$ cells in vitro. F. W. Pagliuca et al. Cell 2014 oct

Abstract

The generation of insulin-producing pancreatic $\beta$ cells from stem cells in vitro would provide an unprecedented cell source for drug discovery and cell transplantation therapy in diabetes. However, insulin-producing cells previously generated from human pluripotent stem cells (hPSC) lack many functional characteristics of bona fide $\beta$ cells. Here, we report a scalable differentiation protocol that can generate hundreds of millions of glucose-responsive $\beta$ cells from hPSC in vitro. These stem-cell-derived $\beta$ cells (SC-$\beta$) express markers found in mature $\beta$ cells, flux Ca(2+) in response to glucose, package insulin into secretory granules, and secrete quantities of insulin comparable to adult $\beta$ cells in response to multiple sequential glucose challenges in vitro. Furthermore, these cells secrete human insulin into the serum of mice shortly after transplantation in a glucose-regulated manner, and transplantation of these cells ameliorates hyperglycemia in diabetic mice.
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor $\beta$ (TR$\beta$) agonists for the treatment of dyslipidemia. H. Shiohara et al. Bioorganic {\&} medicinal chemistry 2012 jun

Abstract

Thyromimetics that specifically target TR$\beta$ have been shown to reduce plasma cholesterol levels and avoid atherosclerosis through the promotion of reverse cholesterol transport in an animal model. We designed novel thyromimetics with high receptor (TR$\beta$) and organ (liver) selectivity based on the structure of eprotirome (3) and molecular modeling. We found that indane derivatives are potent and dual-selective thyromimetics expected to avoid hypothyroidism in some tissues as well as heart toxicity. KTA-439 (29), a representative indane derivative, showed the same high human TR$\beta$ selectivity in a binding assay as 3 and higher liver selectivity than 3 in a cholesterol-fed rat model.
3,3',5-Triiodo-L-thyronine inhibits ductal pancreatic adenocarcinoma proliferation improving the cytotoxic effect of chemotherapy. S. Michienzi et al. The Journal of endocrinology 2007 may

Abstract

The pancreatic adenocarcinoma is an aggressive and devastating disease, which is characterized by invasiveness, rapid progression, and profound resistance to actual treatments, including chemotherapy and radiotherapy. At the moment, surgical resection provides the best possibility for long-term survival, but is feasible only in the minority of patients, when advanced disease chemotherapy is considered, although the effects are modest. Several studies have shown that thyroid hormone, 3,3',5-triiodo-l-thyronine (T(3)) is able to promote or inhibit cell proliferation in a cell type-dependent manner. The aim of the present study is to investigate the ability of T(3) to reduce the cell growth of the human pancreatic duct cell lines chosen, and to increase the effect of chemotherapeutic drugs at conventional concentrations. Three human cell lines hPANC-1, Capan1, and HPAC have been used as experimental models to investigate the T(3) effects on pancreatic adenocarcinoma cell proliferation. The hPANC-1 and Capan1 cell proliferation was significantly reduced, while the hormone treatment was ineffective for HPAC cells. The T(3)-dependent cell growth inhibition was also confirmed by fluorescent activated cell sorting analysis and by cell cycle-related molecule analysis. A synergic effect of T(3) and chemotherapy was demonstrated by cell kinetic experiments performed at different times and by the traditional isobologram method. We have showed that thyroid hormone T(3) and its combination with low doses of gemcitabine (dFdCyd) and cisplatin (DDP) is able to potentiate the cytotoxic action of these chemotherapic drugs. Treatment with 5-fluorouracil was, instead, largely ineffective. In conclusion, our data support the hypothesis that T(3) and its combination with dFdCyd and DDP may act in a synergic way on adenopancreatic ductal cells.

更多信息

更多信息
Molecular Weight 673 g/mol
Alternative Names Liothyronine; T3; L-3, 3', 5-Triiodothyronine
Cas Number 345957-19-9
Chemical Formula C15H11I3NO4 • Na • XH2O
纯度 ≥ 98%
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