T-26c - MMP-13 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemET-26cCat. No.: HY-100518CAS No.: 869296-13-9分式: CHNOS分量: 479.51作靶点: MMP作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 15.62 mg/mL (32.57 mM; Need ultrasonic)H

2、2O : 40% PEG300 5% Tween-80 45% salineSolubility: 1.56 mg/mL (3.25 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.56 mg/mL (3.25 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 T-26c效和选择性的 质属蛋酶-13 (MMP-13) 抑制剂，IC50 值为6.75 pM。对其他相关属酶的选择性

3、2600倍。IC50 & Target IC50: 6.75 pM (MMP-13) 1体外研究 T-26c significantly inhibits the breakdown of collagen (87.4% inhibition at 0.1 M) in IL-1 and oncostatin Mstimulated cartilage 1.体内研究 T-26c is well absorbed in all species at the oral dose of 1020 mg/kg. Oral administration of the disodium saltformul

4、ations of T-26c to guinea pigs results in significant increases in AUC (8357 ng h/mL) and Cmax (1445ng/ mL) compared with those of the free acid T-26c (AUC = 6478 ng h/ mL and Cmax= 911 ng/mL) 1.REFERENCES1. Nara H, et al. Thieno2,3-dpyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orallyavailable MMP-13 inhibitors interacting with the S1 binding site. Bioorg Med Chem. 2014 Oct 1;22(19):5487-505.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-589559