TD-198946

Research use only, not for human use.

TD-198946, a potent chondrogenic agent, is a thienoindazole derivative.

TD-198946 is a thienoindazole derivative, has been found to be active in the studies as a chondrogenic factor. Cell-sheet technology combined with a thienoindazole derivative small compound TD-198946 for cartilage regeneration. A novel disease-modifying osteoarthritis drug candidate targeting Runx1.

TD-198946 is a potent chondrogenic agent. TD-198946 strongly induces chondrogenic differentiation without promoting hypertrophy in cell and metatarsal organ cultures. TD-198946 induces stronger Col2a1 promoter activity than insulin in ATDC5 cells. In C3H10T1/2 cells, ATDC5 cells and primary mouse chondrocytes, TD-198946 dose-dependently stimulates endogenous expression of the chondrocyte markers Col2a1 and Acan, with maximum effects around 1-10 μM.

When administered directly into the joint space, TD-198946 successfully prevents and repaires degeneration of the articular cartilage. TD-198946 exerts its effect through the regulation of Runx1 expression, which is downregulated in both mouse and human OA cartilage compared with normal tissue. TD-198946 has disease-modifying effects on progressed osteoarthritis. TD-198946 may prevent the progression of osteoarthritis by acting on the remaining chondrocytes rather than repairing damaged cartilage, it may be most effective as a therapeutic during the early or middle stages of osteoarthritis, before the articular cartilage is fully eroded. Cartilaginous cell-sheets are generated by culturing mouse and canine costal chondrocytes and human mesenchymal stem cells with TD-198946 on temperature-responsive dishes. The transplanted cell-sheets are then successfully used to promote the reconstruction of permanent cartilage, with no evidence of chondrocyte hypertrophy in the knee articular cartilage defects created in mice and canines.

TD-198946 | TD 198946 | TD198946

Others

Other Targets

Others

——

——

364762-86-7

482.55

C27H22N4O3S

>98% (HPLC)

DMSO : ≥ 28 mg/mL; 58.03 mM

Cn1c2c(CCc3c(sc(c23)Oc2ccc(cc2)OCc2nc3ccccc3cc2)C(=O)N)cn1

1-Methyl-8-[4-(quinolin-2-ylmethoxy)phenoxy]-4,5-dihydrothieno[3,4-g]indazole-6-carboxamide

(-20℃)

With Ice Pack

≥ 2 years