| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Thyroid hormone receptors TRα and TRβ
Thyroid hormone receptors TRα and TRβ; Liothyronine sodium hydrate is a potent agonist of TRα and TRβ. These receptors are nuclear receptors that regulate gene transcription in response to thyroid hormone. By binding to these receptors, the compound modulates the expression of genes involved in metabolism, growth, differentiation, and development. |
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| ln Vitro |
Liothyronine sodium hydrate interacts to the human thyroid hormone receptor (hTRβ1), causing conformational alterations. Liothyronine sodium hydrate is known to stimulate growth, induce differentiation, and control metabolism [2].
In vitro, Liothyronine sodium hydrate binds to hTRα and hTRβ with Kis of 2.33 nM. It is used in cell-based assays to study thyroid hormone signaling and its effects on cell proliferation, differentiation, and metabolism. It promotes pancreatic β-cell differentiation from human pluripotent stem cells and inhibits the proliferation of pancreatic adenocarcinoma cells. |
| ln Vivo |
In vivo, Liothyronine sodium hydrate is used to study thyroid hormone function. It is administered to animal models to investigate its effects on metabolism, growth, and development. It is also used in research on hypothyroidism, stroke, and cognitive dysfunction.
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| Enzyme Assay |
To understand the structural basis in the hormone-dependent transcriptional regulation of human beta 1 thyroid hormone receptor (h-TR beta 1), we studied the conformational changes of h-TR beta 1 induced by binding of 3,3',5-triiodo-L-thyronine (T3). h-TR beta 1 was treated with trypsin alone or in the presence of T3, thyroid hormone response element (TRE) or T3 together with TREs. Without T3, h-TR beta 1 was completely digested by trypsin. Binding of TREs had no effect on the tryptic digestion pattern. However, T3-bound h-TR beta 1 became resistant to tryptic digestion and yielded trypsin-resistant peptide fragments with molecular weight of 28,000 and 24,000. Chymotryptic digestion also yielded a T3-protected 24 Kd peptide fragment. Using anti-h-TR beta 1 antibodies and amino acid sequencing, the 28 Kd fragment was identified to be Ser202-Asp456. The 24 Kd tryptic fragments were found to be Lys239-Asp456 and Phe240-Asp456. The 24 Kd chymotryptic fragment was identified to be Lys235-Asp456. The structural changes as a result of T3 binding could serve as a transducing signal to modulate the gene regulating activity of h-TR beta 1[2].
In vitro, the binding affinity of Liothyronine sodium hydrate to TRα and TRβ is measured using radioligand binding assays. The Ki values of 2.33 nM for both receptors are determined. Cell-based assays are used to study its effects on gene expression and cellular function. |
| Cell Assay |
To understand the role of thyroid hormone nuclear receptors (TRs) in hepatocarcinogenesis, we characterized the TRs in nine human hepatocarcinoma cell lines. The expression of TR proteins is receptor subtype- and cell type-dependent. TR alpha 1 protein expresses similarly at a low level in each of the nine cell lines. In contrast, TR beta 1 is overexpressed in hepatocarcinoma cells which are poorly differentiated. Furthermore, thyroid hormone was found to stimulate the proliferation of cells in which TR beta 1 is overexpressed. These results suggest that TR beta 1 is most likely involved in the differentiation and proliferation of hepatocarcinoma cells. Our studies have shed new light in the understanding of the role of TRs in liver carcinogenesis[1].
In cell-based assays, various cell types are treated with Liothyronine sodium hydrate. The compound is typically dissolved in DMSO or water. Effects on cell proliferation, differentiation, and gene expression are assessed. For example, it is used to promote pancreatic β-cell differentiation from human pluripotent stem cells. |
| Animal Protocol |
In vivo, Liothyronine sodium hydrate is administered to animal models via oral or intravenous routes. The animals are monitored for changes in metabolic parameters, body weight, and neurological function. It is used in research on hypothyroidism and other conditions.
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| ADME/Pharmacokinetics |
Liothyronine sodium hydrate has a molecular weight of 690.97 and formula C15H13I3NNaO5. It is soluble in water. Storage: Store at -20°C, protected from light.
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| Toxicity/Toxicokinetics |
Specific toxicity data are not extensively documented. As a thyroid hormone analog, it can have significant effects on metabolism and cardiovascular function at high doses. The compound is for research use only.
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| References |
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| Additional Infomation |
Liothyronine sodium is the sodium salt of Liothyronine. Liothyronine sodium is considered to be more active than levothyroxine, with a rapid onset of action (within hours) and a shorter duration of action. It is used to treat hypothyroidism, especially hypothyroid coma. It contains 3,3',5-triiodo-L-thyroxine salt. Liothyronine sodium is the sodium salt form of Liothyronine, the synthetic form of the levorotatory isomer of the natural thyroid hormone triLiothyronine (T3). Liothyronine sodium binds to the nuclear thyroid receptor, which in turn binds to the thyroid hormone response element of the target gene. Therefore, Liothyronine sodium induces the expression of genes required for normal growth and development. Liothyronine sodium is more potent and has a faster onset of action than thyroxine (T4). Thyroid hormone T3 is normally synthesized and secreted by the thyroid gland, but its content is much lower than that of thyroxine (T4). Most T3 originates from the single deiodination at the 5' position of the Liothyronine ring in T4. The hormone ultimately transported and utilized by tissues is mainly T3.
Liothyronine sodium hydrate is also known as 3,3',5-Triiodo-L-thyronine sodium salt hydrate and T3 sodium salt. It is an active form of thyroid hormone and a potent TRα and TRβ agonist. |
| Molecular Formula |
C15H11NO4I3-.NA+.H2O
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|---|---|
| Molecular Weight |
690.96922
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| Exact Mass |
690.783
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| CAS # |
345957-19-9
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| Related CAS # |
Liothyronine sodium;55-06-1;Liothyronine;6893-02-3;Liothyronine hydrochloride;6138-47-2
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| PubChem CID |
23687509
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| Appearance |
White to light brown solid powder
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| Melting Point |
205ºC (dec.)(lit.)
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| LogP |
5.026
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
408
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O.[Na+].O=C([C@H](CC1C=C(I)C(OC2C=CC(O)=C(I)C=2)=C(I)C=1)N)[O-]
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| InChi Key |
IRGJMZGKFAPCCR-LTCKWSDVSA-M
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| InChi Code |
InChI=1S/C15H12I3NO4.Na.H2O/c16-9-6-8(1-2-13(9)20)23-14-10(17)3-7(4-11(14)18)5-12(19)15(21)22;;/h1-4,6,12,20H,5,19H2,(H,21,22);;1H2/q;+1;/p-1/t12-;;/m0../s1
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| Chemical Name |
sodium;(2S)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoate;hydrate
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| Synonyms |
3,3',5-Triiodo-L-thyronine sodium salt hydrate; 3 3' 5-TRIIODO-L-THYRONINE SODIUM SALT&; sodium;(2S)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoate;hydrate; 3 3' 5-TRIIODO-L-THYRONINE SODIUM SALT&; SCHEMBL41655; MLS001333755; CHEMBL1356342; .
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4472 mL | 7.2362 mL | 14.4724 mL | |
| 5 mM | 0.2894 mL | 1.4472 mL | 2.8945 mL | |
| 10 mM | 0.1447 mL | 0.7236 mL | 1.4472 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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