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Levothyroxine sodium.

(Synonyms: 左甲状腺素钠; Levothyroxine sodium; T4 sodium)
目录号: PC19180 纯度: ≥98%
L-Thyroxine sodium (Levothyroxine sodium) 是一种合成的甲状腺激素,用于甲状腺功能减退症的研究。DIO 酶将 L-Thyroxine (T4) 转化成具有生物活性的三碘甲状腺氨酸 (T3)。
CAS No. :55-03-8
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中文名称
Levothyroxine sodium.
中文别名
左甲状腺素钠;左旋甲状腺素钠;甲碘四安钠盐;甲状腺素;L-甲状腺素钠盐五水合物;L-Thyroxine Sodium Salt Pentahydrate L-甲状腺素钠盐五水合物;L-甲状腺素钠;左甲状腺素钠粉;左旋甲状腺素钠 水合物;L-甲状腺素钠五水合物;small>-甲状腺素钠盐五水合物;(S)-2-氨基-3-[4-(4-羟基-3,5-二碘苯氧基)-3,5-二碘苯基]丙酸钠盐 五水合物;湖北扬信现货供应左甲状腺素钠杂质ABCDE
英文名称
12,18,30,36,50,56-Hexamethyl-22,40,60-tris(4-methylphenyl)-8,22,26,40,46,60-hexaza-5lambda5-phosphaoctadecacyclo[44.14.2.17,23.113,17.131,35.141,45.151,55.03,8.04,62.05,44.06,25.09,14.016,21.026,43.027,32.034,39.047,52.054,59]heptahexaconta-1(61),2,4(62),6,9,11,13(67),14,16(21),17,19,23(66),24,27,29,31(65),32,34(39),35,37,41,43,45(64),47,49,51(63),52,54(59),55,57-triacontaene 5-oxide
英文别名
L-Thyroxine sodium;Thyroxinesodiumsalt;L-Thyroxine sodium salt;sodium 4-o-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-l-tyrosine;Sodium Levothyroxine;Levothyroxine sodium;Levothyroxine sodium hydrate;Thyroxine;(S)-2-Amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propionic Acid Sodium Salt Pentahydrate;L<;Sodium (S)-2-Amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propionate Pentahydrate;12,18,30,36,50,56-Hexamethyl-22,40,60-tris(4-methylphenyl)-5-sulfanylidene-8,22,26,40,46,60-hexaza-5;12,18,30,36,50,56-Hexamethyl-22,40,60-tris(4-methylphenyl)-8,22,26,40,46,60-hexaza-5lambda5-phosphao
Cas No.
55-03-8
分子式
C87H63N6OP
分子量
1239.44
包装储存

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

详情描述

L-Thyroxine sodium (Levothyroxine sodium) 是一种合成的甲状腺激素,用于甲状腺功能减退症的研究。DIO 酶将 L-Thyroxine (T4) 转化成具有生物活性的三碘甲状腺氨酸 (T3)。

生物活性

L-Thyroxine sodium (Levothyroxine sodium) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).

性状

Solid

IC50 & Target[1][2]

Human Endogenous Metabolite

 

体内研究(In Vivo)

Deiodinases (DIOs), which catalyse the conversion of thyroxine (pro-hormone) to the active thyroid hormone, are associated with thyroid stimulating hormone (TSH) levels. DIO1 and DIO2 catalyze activation of thyroid hormone secretion in contrast to DIO3 playing role inactivation of the secretion. Activities of DIO1 and DIO2 play pivotal role in the negative feedback regulation of pituitary TSH secretion. L-Thyroxine (T4) and Triiodothyronine (T3) hormones are known to modulate the expression of ionic channels, pumps and regulatory contractile proteins. Moreover, thyroid hormones have been shown to influence calcium homeostasis and flux responsible for excitation and contractility, with L-Thyroxine and Triiodothyronine modulating its pharmacological control and secretion. In rats fed 12 weeks with the iodine-free diet, a significant decrease in the levels of both Triiodothyronine and L-Thyroxine is observed when compared to the control group fed with standard diet (p<0.001). In the group treated with low doses of L-Thyroxine, an increase in L-Thyroxine levels is observed (p=0.02) while Triiodothyronine levels remain virtually similar to the control group (p=0.19). Rats treated with high doses of L-Thyroxine display a significant increase in both Triiodothyronine and L-Thyroxine circulating concentrations compared to the non-treated hypothyroid group (p<0.001 and p=0.004, respectively) and a significant increase in L-Thyroxine levels when compared to the control values (p=0.03).

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 62.5 mg/mL (78.24 mM; Need ultrasonic)

0.5 M NaOH : 25 mg/mL (31.29 mM; ultrasonic and warming and adjust pH to 11 with NaOH and heat to 60°C)

H2O : 14 mg/mL (17.53 mM; ultrasonic and adjust pH to 12 with NaOH)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2518 mL 6.2590 mL 12.5180 mL
5 mM 0.2504 mL 1.2518 mL 2.5036 mL
10 mM 0.1252 mL 0.6259 mL 1.2518 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.60 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.60 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.60 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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