Eprotirome - CAS 355129-15-6
Catalog number:
355129-15-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H17Br2NO5
Molecular Weight:
487.14
COA:
Inquire
Targets:
Others
Description:
Eprotirome is a synthetic thyroid hormone mimetic as a thyroid hormone receptor beta agonists, lowers total and low-density lipoprotein cholesterol up to 40% without affecting high-density lipoprotein cholesterol levels and without deleterious side effects to the cardiovascular system.
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Purity:
≥98%
Appearance:
White powder
Synonyms:
KB2115; 3-[[3,5-dibromo-4-[4-hydroxy-3-(1-methylethyl)phenoxy]phenyl]amino-3-oxo-propanoic acid;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Thyroid hormone receptor beta agonists
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
Boiling Point:
596.315ºC at 760 mmHg
Density:
1.708
InChIKey:
VPCSYAVXDAUHLT-UHFFFAOYSA-N
InChI:
1S/C18H17Br2NO5/c1-9(2)12-7-11(3-4-15(12)22)26-18-13(19)5-10(6-14(18)20)21-16(23)8-17(24)25/h3-7,9,22H,8H2,1-2H3,(H,21,23)(H,24,25)
Canonical SMILES:
CC(C)C1=C(C=CC(=C1)OC2=C(C=C(C=C2Br)NC(=O)CC(=O)O)Br)O
Current Developer:
Karo Bio
1.Reductions in serum levels of LDL cholesterol, apolipoprotein B, triglycerides and lipoprotein(a) in hypercholesterolaemic patients treated with the liver-selective thyroid hormone receptor agonist eprotirome.
Angelin B1, Kristensen JD, Eriksson M, Carlsson B, Klein I, Olsson AG, Chester Ridgway E, Ladenson PW. J Intern Med. 2015 Mar;277(3):331-42. doi: 10.1111/joim.12261. Epub 2014 May 16.
BACKGROUND: Liver-selective thyromimetic agents could provide a new approach for treating dyslipidaemia.
2.Thyroid hormone receptor-β agonists prevent hepatic steatosis in fat-fed rats but impair insulin sensitivity via discrete pathways.
Vatner DF1, Weismann D, Beddow SA, Kumashiro N, Erion DM, Liao XH, Grover GJ, Webb P, Phillips KJ, Weiss RE, Bogan JS, Baxter J, Shulman GI, Samuel VT. Am J Physiol Endocrinol Metab. 2013 Jul 1;305(1):E89-100. doi: 10.1152/ajpendo.00573.2012. Epub 2013 May 7.
Liver-specific thyroid hormone receptor-β (TRβ)-specific agonists are potent lipid-lowering drugs that also hold promise for treating nonalcoholic fatty liver disease and hepatic insulin resistance. We investigated the effect of two TRβ agonists (GC-1 and KB-2115) in high-fat-fed male Sprague-Dawley rats treated for 10 days. GC-1 treatment reduced hepatic triglyceride content by 75%, but the rats developed fasting hyperglycemia and hyperinsulinemia, attributable to increased endogenous glucose production (EGP) and diminished hepatic insulin sensitivity. GC-1 also increased white adipose tissue lipolysis; the resulting increase in glycerol flux may have contributed to the increase in EGP. KB-2115, a more TRβ- and liver-specific thyromimetic, also prevented hepatic steatosis but did not induce fasting hyperglycemia, increase basal EGP rate, or diminish hepatic insulin sensitivity. Surprisingly, insulin-stimulated peripheral glucose disposal was diminished because of a decrease in insulin-stimulated skeletal muscle glucose uptake.
3.The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivity in ob/ob mice.
Martagón AJ1, Lin JZ2, Cimini SL3, Webb P3, Phillips KJ3. PLoS One. 2015 Apr 7;10(4):e0122987. doi: 10.1371/journal.pone.0122987. eCollection 2015.
Thyroid hormone receptor (TR) agonists have been proposed as therapeutic agents to treat non-alcoholic fatty liver disease (NAFLD) and insulin resistance. We investigated the ability of the TR agonists GC-1 and KB2115 to reduce hepatic steatosis in ob/ob mice. Both compounds markedly reduced hepatic triglyceride levels and ameliorated hepatic steatosis. However, the amelioration of fatty liver was not sufficient to improve insulin sensitivity in these mice and reductions in hepatic triglycerides did not correlate with improvements in insulin sensitivity or glycemic control. Instead, the effects of TR activation on glycemia varied widely and were found to depend upon the time of treatment as well as the compound and dosage used. Lower doses of GC-1 were found to further impair glycemic control, while a higher dose of the same compound resulted in substantially improved glucose tolerance and insulin sensitivity, despite all doses being equally effective at reducing hepatic triglyceride levels.
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CAS 355129-15-6 Eprotirome

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