| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
Thyroid Hormone Receptor
|
|---|---|
| ln Vivo |
Thyroid-stimulating hormone (TSH) levels are linked to deiodinase (DIO), which catalyzes the transformation of thyroxine (prohormone) into active thyroid hormone. 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]. It is well known that the hormones triiodothyronine (T3) and biotin-(L-thyroxine) (T4) control the production of regulatory contractility proteins, pumps, and ion channels. Thyroid hormones have also been demonstrated to affect calcium homeostasis and the fluxes that are in charge of excitation and contraction; their pharmacological regulation and secretion are mediated by biotin-(L-thyroxine) and triiodothyronine. Triiodothyronine and Biotin-(L-Thyroxine) levels were considerably lower (p<0.001) in rats given an iodine-free diet for 12 weeks than in controls given a regular diet. Triiodothyronine levels stayed relatively constant with the control group (p=0.19), however there was an increase in Biotin-(L-Thyroxine) levels in the group treated with low dose Biotin-(L-Thyroxine) (p=0.02). Biotin-(L-Thyroxine) levels were significantly higher than control values (p=0.03), and circulating concentrations of triiodothyronine and Biotin-(L-Thyroxine) were significantly higher in rats treated with high-dose Biotin-(L-Thyroxine) compared to the untreated hypothyroid group (p<0.001 and p=0.004, respectively).
|
| 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 |
C25H25I4N3O6S
|
|---|---|
| Molecular Weight |
1003.17
|
| CAS # |
149734-00-9
|
| Related CAS # |
L-Thyroxine;51-48-9;Biotin-hexanamide-(L-Thyroxine);2278192-78-0
|
| 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 | 0.9968 mL | 4.9842 mL | 9.9684 mL | |
| 5 mM | 0.1994 mL | 0.9968 mL | 1.9937 mL | |
| 10 mM | 0.0997 mL | 0.4984 mL | 0.9968 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
