For research use only. Not for therapeutic Use.
Ertiprotafib (Cat.No:I006707), also known as PTP-112, is a Protein Tyrosine Phosphatase 1B Inhibitor (PTP1B inhibitor). Ertiprotafib normalized the plasma glucose and insulin levels in diabetic animal models, and progressed to a phase II clinical trial. Ertiprotafib is potentially useful for the treatment of Non-Insulin Dependent Diabetes. Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta), with an IC(50) of 400nM.
| Catalog Number | I006707 |
| CAS Number | 251303-04-5 |
| Synonyms | PTP-112; PTP112; PTP 112; Ertiprotafib.;(2R)-2-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thiophen-4-yl)-2,6-dimethylphenoxy)-3-phenylpropionic acid |
| Molecular Formula | C31H27BrO3S |
| Purity | ≥95% |
| Target | NF-κB |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20 °C |
| IUPAC Name | (2R)-2-[4-(9-bromo-2,3-dimethylbenzo[f][1]benzothiol-4-yl)-2,6-dimethylphenoxy]-3-phenylpropanoic acid |
| InChI | InChI=1S/C31H27BrO3S/c1-17-14-22(15-18(2)29(17)35-25(31(33)34)16-21-10-6-5-7-11-21)27-23-12-8-9-13-24(23)28(32)30-26(27)19(3)20(4)36-30/h5-15,25H,16H2,1-4H3,(H,33,34)/t25-/m1/s1 |
| InChIKey | FONCZICQWCUXEB-RUZDIDTESA-N |
| SMILES | CC1=CC(=CC(=C1OC(CC2=CC=CC=C2)C(=O)O)C)C3=C4C(=C(SC4=C(C5=CC=CC=C53)Br)C)C |
| Reference | </br>1:Discovery of novel PTP1B inhibitors via pharmacophore-oriented scaffold hopping from Ertiprotafib. Liu JZ, Zhang SE, Nie F, Yang Y, Tang YB, Yin W, Tian JY, Ye F, Xiao Z.Bioorg Med Chem Lett. 2013 Dec 1;23(23):6217-22. doi: 10.1016/j.bmcl.2013.10.002. Epub 2013 Oct 8. PMID: 24148325 </br>2:PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta). Shrestha S, Bhattarai BR, Cho H, Choi JK, Cho H.Bioorg Med Chem Lett. 2007 May 15;17(10):2728-30. Epub 2007 Mar 3. PMID: 17407812 </br>3:Effects of ertiprotafib on hepatic cytochrome P450 and peroxisomal enzymes in rats and dogs, and in rat and human primary hepatocytes. Tong Z, Chandrasekaran A, Jordan R, Markiewicz V, Li H, Xiang Q, Shen L, Scatina J.Xenobiotica. 2007 Jan;37(1):1-18. PMID: 17178630 </br>4:Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Erbe DV, Wang S, Zhang YL, Harding K, Kung L, Tam M, Stolz L, Xing Y, Furey S, Qadri A, Klaman LD, Tobin JF.Mol Pharmacol. 2005 Jan;67(1):69-77. Epub 2004 Oct 8. PMID: 15475571 Free Article |
