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Levothyroxine (L-Thyroxine) sodium THR agonist

Name: Levothyroxine (L-Thyroxine) sodium
Brand: Selleck Chemicals
SKU: S3747
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3747

Levothyroxine (L-Thyroxine) sodium is the major hormone derived from the thyroid gland. It is the agonist of Thyroid hormone receptor alpha and beta.

Chemical Structure

Molecular Weight: 798.85

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	T3 (Triiodothyronine) Resmetirom (MGL-3196)

Chemical Information, Storage & Stability

Molecular Weight	798.85	Formula	C₁₅H₁₀I₄NO₄.Na	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	55-03-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (125.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (6.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (6.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Levothyroxine can upregulate the expression of P-gp mRNA and protein in LS180 cells and can produce the same effect in Caco-2 cells, which are relatively lacking in PXR. It doea not affect the expression of CYP3A4 in either cell line^[1].
In vivo	Levothyroxine is a synthetic T4 hormone that is biochemically and physiologically indistinguishable from the natural one, and it is administered when the body is deficient in the natural hormone. Its nain site of absorption is small intestine, more specifically through the duodenum, jejunum and ileum. Very little is absorbed in the stomach. The bioavailability is about 70-80 % in euthyroid person and may be slightly higher in hyperthyroid patients. The absorption of levothyroxine appears to be influenced by gastric pH. Tmax=2-3 hours and the half-time T_1/2 is 6.2 and 7.5 days in euthyroid and hypothyroid patients, respectively^[3]. T4 hormones is known to modulate the expression of ionic channels, pumps and regulatory contractile proteins. T4-treatment induces a dose-dependent increase in the duration of contractions. Abnormal uterine contractile pattern are induced by T4-treatment^[2].
References	https://pubmed.ncbi.nlm.nih.gov/15258100/ http://www.sciencedirect.com/science/article/pii/S2214623714000374 http://www.touchendocrinology.com/articles/review-pharmacokinetics-levothyroxine-treatment-hypothyroidism/page/3/0

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04037748	Completed	Healthy	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany	June 25 2019	Phase 1

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