Eprotirome

• CAT Number: I006693
• CAS Number: 355129-15-6
• Molecular Formula: C18H17Br2NO5
• Molecular Weight: 487.144
• Purity: ≥95%
• Target: thyroid hormone receptor agonist
• Solubility: Soluble in DMSO, not in water
• Storage: -20°C
• IUPAC Name: 3-[3,5-dibromo-4-(4-hydroxy-3-propan-2-ylphenoxy)anilino]-3-oxopropanoic acid
• InChI: 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)
• InChIKey: VPCSYAVXDAUHLT-UHFFFAOYSA-N
• SMILES: CC(C)C1=C(C=CC(=C1)OC2=C(C=C(C=C2Br)NC(=O)CC(=O)O)Br)O

Eprotirome (CAT: I006693) is a synthetic thyroid hormone receptor agonist that selectively activates thyroid hormone receptor β (TRβ) and inhibits TRα. It has been developed as a potential treatment for dyslipidemia and metabolic syndrome. Eprotirome has shown beneficial effects on lipid profiles by increasing high-density lipoprotein (HDL) cholesterol and reducing low-density lipoprotein (LDL) cholesterol and triglyceride levels. It also has the potential to improve insulin sensitivity and promote weight loss. However, further research is needed to fully evaluate its efficacy and safety for clinical use.

Overview of Clinical Research

Eprotirome is a thyroid hormone receptor beta agonist.

Reference

1:The thyromimetic KB2115 (Eprotirome) induces rat hepatocyte proliferation. Szydlowska M, Pibiri M, Perra A, Puliga E, Mattu S, Ledda-Columbano GM, Columbano A, Leoni VP.Gene Expr. 2017 Apr 13. doi: 10.3727/105221617X695438. [Epub ahead of print] PMID: 28409553
2:The Thyroid Hormone Analogue KB2115 (Eprotirome) Prolongs Human Hair Growth (Anagen) Ex Vivo. Oláh A, Gherardini J, Bertolini M, Chéret J, Ponce L, Kloepper J, Bíró T, Soeberdt M, Abels C, Paus R.J Invest Dermatol. 2016 Aug;136(8):1711-4. doi: 10.1016/j.jid.2016.03.033. Epub 2016 Apr 8. No abstract available. PMID: 27066887
3: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 B, 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. PMID: 24754313 Free Article
4:Eprotirome in patients with familial hypercholesterolaemia (the AKKA trial): a randomised, double-blind, placebo-controlled phase 3 study. Sjouke B, Langslet G, Ceska R, Nicholls SJ, Nissen SE, Öhlander M, Ladenson PW, Olsson AG, Hovingh GK, Kastelein JJ.Lancet Diabetes Endocrinol. 2014 Jun;2(6):455-63. doi: 10.1016/S2213-8587(14)70006-3. Epub 2014 Feb 18. PMID: 24731671
5:Lipids: Eprotirome shows promise as a novel way to target dyslipidemia. Koch L.Nat Rev Endocrinol. 2010 Jul;6(7):354. doi: 10.1038/nrendo.2010.74. No abstract available. PMID: 20583340
6:Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. Ladenson PW, Kristensen JD, Ridgway EC, Olsson AG, Carlsson B, Klein I, Baxter JD, Angelin B.N Engl J Med. 2010 Mar 11;362(10):906-16. doi: 10.1056/NEJMoa0905633. PMID: 20220185 Free Article