| Identification | Back Directory | [Name]
TD-198946 | [CAS]
364762-86-7 | [Synonyms]
TD-198946
TD-198946, >98%
TD198946;TD 198946
1-(3-PYRIDINYLMETHYL)-4-PIPERIDINOL DIHYDROCHLORIDE
4,5-dihydro-1-methyl-8-[4-(2-quinolinylmethoxy)phenoxy]-1H-thieno[3,4-g]indazole-6-carboxamide
1-Methyl-8-[4-(2-quinolinylmethoxy)phenoxy]-4,5-dihydro-1H-thieno [3,4-g]indazole-6-carboxamide
1H-Thieno[3,4-g]indazole-6-carboxamide, 4,5-dihydro-1-methyl-8-[4-(2-quinolinylmethoxy)phenoxy]-
TD-198946 (1-methyl-8-[4-(2-quinolinylmethoxy)phenoxy]-4,5-dihydro-1h-thieno [3,4-g]indazole-6-carboxamide) | [Molecular Formula]
C27H22N4O3S | [MDL Number]
MFCD28044311 | [MOL File]
364762-86-7.mol | [Molecular Weight]
482.55 |
| Chemical Properties | Back Directory | [Boiling point ]
699.5±55.0 °C(Predicted) | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
15.87±0.20(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
TD-198946, a thienoindazole derivative, is a potent chondrogenic agent. | [Biological Activity]
TD-198946 is a thienoazole derivative,it is a highly potent cartilage-forming agent. | [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.It exerts its effect through the regulation of Runx1 expression, which is downregulated in both mouse and human OA cartilage compared with normal tissue.It has disease-modifying effects on progressed osteoarthritis.It 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. | [References]
[1] Yano F, et al. A novel disease-modifying osteoarthritis drug candidate targeting Runx1. Ann Rheum Dis. 2013 May;72(5):748-53. DOI:10.1136/annrheumdis-2012-201745
[2] Yano F, et al. Disease-modifying effects of TD-198946 on progressed osteoarthritis in a mouse model. Ann Rheum Dis. 2014 Nov;73(11):2062-4. DOI:10.1136/annrheumdis-2014-205672
[3] Yano F, et al. Cell-sheet technology combined with a thienoindazole derivative small compound TD-198946 for cartilage regeneration. Biomaterials. 2013 Jul;34(22):5581-7. DOI:10.1016/j.biomaterials.2013.04.008
[4] Kobayashi M, Chijimatsu R, Hart DA, et al. Evidence that TD-198946 enhances the chondrogenic potential of human synovium-derived stem cells through the NOTCH3 signaling pathway. J Tissue Eng Regen Med. 2021;15(2):103-115. DOI:10.1002/term.3149 |
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BOC Sciences
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www.bocsci.com |
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