| Bioactivity | T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes[1]. | ||||||||||||
| Target | IC50: 6.75 pM (MMP-13) | ||||||||||||
| Invitro | T-26c significantly inhibits the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1β and oncostatin M stimulated cartilage[1]. | ||||||||||||
| In Vivo | T-26c is well absorbed in all species at the oral dose of 10–20 mg/kg. Oral administration of the disodium salt formulations of T-26c to guinea pigs results in significant increases in AUC (8357 ng h/mL) and Cmax (1445 ng/ mL) compared with those of the free acid T-26c (AUC = 6478 ng h/ mL and Cmax= 911 ng/mL)[1]. | ||||||||||||
| Name | T-26c | ||||||||||||
| CAS | 869296-13-9 | ||||||||||||
| Formula | C24H21N3O6S | ||||||||||||
| Molar Mass | 479.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Nara H, et al. Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site. Bioorg Med Chem. 2014 Oct 1;22(19):5487-505. |