规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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靶点 |
Endogenous Metabolite
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体外研究 (In Vitro) |
d-甲状腺素(d-T4)是合成l-T4的副产物,在甲状腺中没有活性。
二羟基香豆素的药理作用也受到D-甲状腺素钠的影响[2]。
D-甲状腺素是甲状腺素的D-对映异构体。它是一种甲状腺素和D-酪氨酸衍生物。它是L-甲状腺素的对映体。 甲状腺分泌的主要激素。甲状腺素是通过酪氨酸的碘化(单碘酪氨酸)和甲状腺球蛋白中碘酪氨酸的偶联(二碘酪氨酸)合成的。甲状腺素通过蛋白水解从甲状腺球蛋白中释放出来,分泌到血液中。甲状腺素在外周脱碘形成三碘甲状腺原氨酸,对细胞代谢产生广泛的刺激作用。 右甲状腺素是甲状腺素的右旋异构体,甲状腺素是一种具有抗高脂血症活性的甲状腺激素。右甲状腺素刺激低密度脂蛋白(LDL)的形成,并增加LDL的分解代谢,从而导致胆固醇和胆汁酸通过胆道途径的排泄增加。这导致血清胆固醇和LDL降低。 |
体内研究 (In Vivo) |
D-甲状腺素钠可降低小鼠体内戊巴比妥、哌替啶和二羟基香豆素的代谢[1]。
在小鼠中,D-甲状腺素抑制双羟基香豆素以及哌替啶和戊巴比妥的代谢;在人体中,在不改变药物代谢速率的剂量下,对双羟基香豆素的抗凝反应会增加。氯贝特不会影响小鼠或人体内的双羟基香豆素代谢,但会增加人体对药物的抗凝反应。去甲屈龙也会增加人体内对双羟基香豆素的抗凝反应,而不影响药物的代谢速率。由于这三种药物的临床有效剂量不会降低维生素K依赖性凝血因子的浓度,也不会影响双羟基香豆素在人体内的吸收、分布或代谢,因此它们似乎可能通过增加受体部位对抗凝剂的亲和力来增强双羟基香豆素的药理作用[1]。 |
酶活实验 |
用于测定d-T4的电流型生物传感器[2]
将石蜡油和石墨粉末以1:4(w/w)的比例混合以形成石墨糊。将100微升l-氨基酸氧化酶(l-AAOD)(EC 1.4.3.2,I型:金刚石斛粗干毒液)的酶溶液(1 mg酶ml−1,0.1 mol l−1磷酸盐缓冲液,pH 7.0)加入碳糊中。塑料尖端填充有相应的石墨-石蜡油糊,在顶部留下3-4mm的空白,填充有含有酶的碳糊。传感器的直径为3mm。通过将银线插入碳糊中获得电接触。电极尖端在细纸上轻轻摩擦,以产生平坦的表面。电极表面用去离子水润湿,然后在使用前用氧化铝纸(抛光条30144-001)抛光。生物传感器在4°C下干燥储存。 |
动物实验 |
In mice, D-thyroxine inhibits the metabolism of bishydroxycoumarin as well as that of meperidine and pentobarbital; in man, the anticoagulant response to bishydroxycoumarin is increased at doses which do not change the rate of metabolism of the drug. Clofibrate does not affect bishydroxycoumarin metabolism in mice or in man but does increase the anticoagulant response to the drug in man. Norethandrolone also increases the anticoagulant response to bishydroxycoumarin in man without affecting the rate of metabolism of the drug. Since clinically effective doses of these three drugs do not decrease the concentration of vitamin K-dependent clotting factors or affect the absorption, distribution, or metabolism of bishydroxycoumarin in man, it seems likely that they potentiate the pharmacologic effect of bishydroxycoumarin by increasing the affinity of the receptor site for the anticoagulant [1].
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毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Thyroid is an animal-derived mixture of levothyroxine (T4) and liothyronine (T3), which are normal components of human milk. Limited data on exogenous replacement doses of levothyroxine during breastfeeding indicate no adverse effects in infants. If thyroid is required by the mother, it is not a reason to discontinue breastfeeding. The American Thyroid Association recommends that subclinical and overt hypothyroidism should be treated with levothyroxine in lactating women seeking to breastfeed. Thyroid dosage requirement may be increased in the postpartum period compared to prepregnancy requirements patients with Hashimoto's thyroiditis. ◉ Effects in Breastfed Infants Effects of exogenous thyroid hormone administration to mothers on their infant have not been reported. One case of apparent mitigation of cretinism in hypothyroid infants by breastfeeding has been reported, but the amounts of thyroid hormones in milk are not optimal, and this result has been disputed. The thyroid hormone content of human milk from the mothers of very preterm infants appears not to be sufficient to affect the infants' thyroid status. The amounts of thyroid hormones in milk are apparently not sufficient to interfere with diagnosis of hypothyroidism. In a telephone follow-up study, 5 nursing mothers reported taking levothyroxine (dosage unspecified). The mothers reported no adverse reactions in their infants. One mother with who had undergone a thyroidectomy was taking levothyroxine 100 mcg daily as well as calcium carbonate and calcitriol. Her breastfed infant was reportedly "thriving" at 3 months of age. ◉ Effects on Lactation and Breastmilk Adequate thyroid hormone serum levels are required for normal lactation. Replacing deficient thyroid levels should improve milk production caused by hypothyroidism. Supraphysiologic doses would not be expected to further improve lactation. |
参考文献 |
[1]. John J. Schrogie M.D., et al. II. The effect of D-thyroxine, clofibrate, and norethandrolone. Clinical Pharmacology and Therapeutics, Volume8, Issue1part1 January 1967 Pages 70-77
[2]. Raluca-IoanaStefan, et al. Simultaneous determination of l-thyroxine (l-T4), d-thyroxine (d-T4), and l-triiodothyronine (l-T3) using a sensors/sequential injection analysis system. |
其他信息 |
The dextrorotary isomer of the synthetic THYROXINE.
See also: Dextrothyroxine Sodium (annotation moved to). |
分子式 |
C15H10NO4I4-.NA+
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分子量 |
798.850000000001
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精确质量 |
798.669
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元素分析 |
C, 22.55; H, 1.26; I, 63.54; N, 1.75; Na, 2.88; O, 8.01
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CAS号 |
137-53-1
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相关CAS号 |
D-Thyroxine;51-49-0
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PubChem CID |
23690433
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外观&性状 |
Solid powder
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沸点 |
576.3ºC at 760mmHg
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闪点 |
302.3ºC
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蒸汽压 |
4.02E-14mmHg at 25°C
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LogP |
3.922
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tPSA |
95.61
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氢键供体(HBD)数目 |
2
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氢键受体(HBA)数目 |
5
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可旋转键数目(RBC) |
5
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重原子数目 |
25
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分子复杂度/Complexity |
426
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定义原子立体中心数目 |
1
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SMILES |
[Na+].O=C(C(CC1C=C(I)C(OC2C=C(I)C(O)=C(I)C=2)=C(I)C=1)N)[O-]
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InChi Key |
YDTFRJLNMPSCFM-UTONKHPSSA-M
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InChi Code |
InChI=1S/C15H11I4NO4.Na/c16-8-4-7(5-9(17)13(8)21)24-14-10(18)1-6(2-11(14)19)3-12(20)15(22)23;/h1-2,4-5,12,21H,3,20H2,(H,22,23);/q;+1/p-1/t12-;/m1./s1
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化学名 |
sodium (R)-2-amino-3-(4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl)propanoate
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别名 |
D-Thyroxine sodium salt; 137-53-1; DEXTROTHYROXINE SODIUM; Detyroxin; dynothel; Biotirmone; Choloxin; Debetrol;
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HS Tariff Code |
2934.99.03.00
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO: >10 mM
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溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。