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L-Thyroxine sodium salt pentahydrate is an endogenous thyroid hormone that is produced by the thyroid follicular cells from thyroglobulin. It bears an iodine content.
| Targets |
Human Endogenous Metabolite
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|---|---|
| ln Vitro |
Thyroid stimulating hormone (TSH) levels are linked to deiodinases (DIOs), which catalyze the transformation of thyroxine (pro-hormone) to the active thyroid hormone. While DIO3 plays a role in inactivating the secretion, DIO1 and DIO2 catalyze the activation of thyroid hormone secretion. The negative feedback regulation of pituitary TSH secretion is largely dependent on the activities of DIO1 and DIO2[1]. Ionic channels, pumps, and regulatory contractile proteins are known to have their expression modulated by the hormones triiodothyronine (T3) and levothyroxine (T4). Additionally, it has been demonstrated that thyroid hormones affect the calcium flux and homeostasis that are in charge of excitation and contractility, with L-thyroxine and triiodothyronine influencing the pharmacological regulation and secretion of this process. Rats fed an iodine-free diet for 12 weeks showed a significant reduction in their levels of L-thyroxine and triiodothyronine compared to the control group fed a standard diet (p<0.001). L-thyroxine levels rise (p=0.02) in the group receiving low doses of the medication, but triiodothyronine levels essentially stay the same (p=0.19) as in the control group. Rats given large doses of L-thyroxine show a significant increase in circulating concentrations of both triiodothyronine and L-thyroxine relative to the hypothyroid group that was not treated (p<0.001 and p=0.004, respectively), as well as a significant increase in L-thyroxine levels relative to the control values (p=0.03)[2].
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| ln Vivo |
Thyroid-stimulating hormone (TSH) levels are correlated with the catalysis of thyroxine (prohormone) conversion to active thyroid hormone by deiodinase (DIO). Thyroid hormone secretion is activated by DIO1 and DIO2, whereas secretion is inactivated by DIO3. The regulation of pituitary TSH secretion by negative feedback is largely dependent on the actions of DIO1 and DIO2 [1]. The expression of ion channels, pumps, and regulating contractile proteins is regulated by the hormones triiodothyronine (T3) and L-thyroxine (T4). Moreover, it has been demonstrated that thyroid hormones affect calcium homeostasis and flux, which are in charge of excitation and contraction. Triiodothyronine and L-thyroxine are known to modify the pharmacological regulation and secretion of calcium. Triiodothyronine and L-thyroxine levels significantly decreased (p<0.001) in rats given an iodine-free diet for 12 weeks as compared to controls given a regular diet. Triiodothyronine levels were essentially comparable to those in the control group (p=0.19), but an increase in L-thyroxine was noted in the low-dose L-thyroxine treatment group (p=0.02). Rats treated with high-dose L-thyroxine showed significantly higher circulating concentrations of both triiodothyronine and L-thyroxine compared to the untreated hypothyroid group (p<0.001 and p=0.004, respectively), and L-thyroxine levels were significantly higher than the control value (p=0.03)[2].
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| Animal Protocol |
Rats: The experiment uses 22 female Sprague-Dawley rats. There are four groups of non-pregnant rats: 1) No thyroid function, 2) hypothyroidism, 3) hypothyroidism treated with low doses of L-thyroxine (20 μg/kg/day), and 4) high doses of L-thyroxine (100 μg/kg/day). While the intervention rats (groups 2-4) are fed an iodine-free diet for 12 weeks to induce hypothyroidism, the control group (group 1) is fed a standard diet. This is followed by an additional 4 weeks of feeding to allow for L-thyroxine treatment and screening for hypothyroidism. You have unlimited access to food and water (iodine-free diet). Groups 3 and 4, which represent the hypothyroid group, receive intraperitoneal injections of 20 μg/kg and 100 μg/kg of L-thyroxine per day, respectively, every 24 hours. Within weeks 12 and 16 of starting the iodine-free or control diet, blood samples are taken for thyroid function screening. After treatment, a hysterectomy is performed under general anesthesia (isoflurane 2%), and the two uterine horns are kept in physiological Krebs' solution until isometric tension measurements are taken, which should take no longer than an hour.
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| References |
[1]. Arici M, et al. Association between genetic polymorphism and levothyroxine bioavailability in hypothyroid patients. Endocr J. 2018 Mar 28;65(3):317-323.
[2]. Corriveau S, et al. Levothyroxine treatment generates an abnormal uterine contractility patterns in an in vitro animalmodel. J Clin Transl Endocrinol. 2015 Sep 9;2(4):144-149 |
| Molecular Formula |
C15H20I4NNAO9
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|---|---|
| Molecular Weight |
888.926400000001
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| Exact Mass |
888.7215
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| CAS # |
6106-07-6
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| Related CAS # |
Thyroxine sulfate;77074-49-8;L-Thyroxine;51-48-9;L-Thyroxine sodium;55-03-8
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| Appearance |
Solid
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| SMILES |
C1=C(C=C(C(=C1I)OC2=CC(=C(C(=C2)I)O)I)I)C[C@@H](C(=O)[O-])N.O.O.O.O.O.[Na+]
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| InChi Key |
JMHCCAYJTTWMCX-QWPJCUCISA-M
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| InChi Code |
InChI=1S/C15H11I4NO4.Na.5H2O/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);;5*1H2/q;+1;;;;;/p-1/t12-;;;;;;/m0....../s1
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| Chemical Name |
sodium;(2S)-2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoate;pentahydrate
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| Synonyms |
L-Thyroxine sodium salt pentahydrate; Sodium levothyroxine pentahydrate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
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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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~112.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.81 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1249 mL | 5.6247 mL | 11.2495 mL | |
| 5 mM | 0.2250 mL | 1.1249 mL | 2.2499 mL | |
| 10 mM | 0.1125 mL | 0.5625 mL | 1.1249 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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