TD-198946

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

Product information

CAS Number: 364762-86-7

Molecular Weight: 482.55

Formula: C27H22N4O3S

Chemical Name: 1-methyl-8-{4-[(quinolin-2-yl)methoxy]phenoxy}-1H,4H,5H-thieno[3,4-g]indazole-6-carboxamide

Smiles: CN1N=CC2CCC3=C(SC(OC4=CC=C(C=C4)OCC4=CC=C5C=CC=CC5=N4)=C3C1=2)C(N)=O

InChiKey: QGAMAWMLTUNPAB-UHFFFAOYSA-N

InChi: InChI=1S/C27H22N4O3S/c1-31-24-17(14-29-31)7-13-21-23(24)27(35-25(21)26(28)32)34-20-11-9-19(10-12-20)33-15-18-8-6-16-4-2-3-5-22(16)30-18/h2-6,8-12,14H,7,13,15H2,1H3,(H2,28,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 28 mg/mL (58.03 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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.

Products are for research use only. Not for human use.