Formulation: A solid
Formal Name: N-[(7S)-3-(β-D-glucopyranosyloxy)-5,6,7,9-tetrahydro-1,2-dimethoxy-10-(methylthio)-9-oxobenzo[a]heptalen-7-yl]-acetamide
Purity: ≥98%
Formula Markup: C27H33NO10S
Formula Weight: 563,6
Shelf life (days): 1460
CAS Number: 602-41-5
Notes: Thiocolchicoside is a GABAA receptor antagonist.{62820} It inhibits GABAA receptor-mediated currents in Purkinje cells isolated from rat cerebellum (IC50 = 0.15 µM). It binds strychnine-sensitive glycine receptors in isolated rat spinal cord (IC50 = 1.58 µM).{62818} Thiocolchicoside inhibits cell growth in a panel of cancer cell lines, including KBM5 leukemia and U266 myeloma cells, SCC4 squamous cell carcinoma cells, and HCT116 colon, MCF-7 breast, and A293 kidney cancer cells when used at concentrations ranging from 25 to 100 µM.{62819} It inhibits the anti-apoptotic proteins Bcl-2, X-linked inhibitor of apoptosis (XIAP), myeloid cell leukemia-1 (Mcl-1), Bcl-xL, cIAP-1, and cIAP-2 in KBM5 cells in a concentration-dependent manner. It also inhibits TNF-α-induced NF-κB activation and IκBα degradation in KBM5 cells in a concentration-dependent manner. Formulations containing thiocolchicoside have been used as muscle relaxers in the treatment of rheumatoid arthritis, joint stiffness, and muscle stiffness.
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