TMI-1
CAS No. : 287403-39-8
(Synonyms: WAY-171318)
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $175 | In-stock |
| 25mg | $320 | In-stock |
| 50mg | $450 | In-stock |
| 100mg | $640 | In-stock |
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| Cat. No. : | HY-101448 |
| M.Wt: | 398.50 |
| Formula: | C17H22N2O5S2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 100 mg/mL |
TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions[1][2][3][4].
In Vitro:TMI-1 inhibits TNF-α secretion in mouse monocyte Raw cells with an IC50 of 40 nM, in human monocyte THP-1 cells with an IC50 of 200 nM, in primary human monocyte lines with an IC50 of 190 nM, and in human whole blood with an IC50 of 300 nM[1].
TMI-1 inhibits the shedding of TNFR II in human whole blood, with an IC50 of 0.72μM[1].
TMI-1 (0-20 μM, 5 days) shows a dose-dependent inhibition of proliferation in breast cancer cell lines BT-20, SUM149, MDA-MB-231, SK-BR-3, L226, SUM190, T147D and Cama-1, with ED50 of 1.3, 1.5, 8.1, 1.6, 2.0, 2.0, 2.5, and 2.5 μM respectively, and induces the activity of Caspase-3 and Caspase-7 without affecting the vitality of normal cells[2].
TMI-1 (0-20 μM, 48 h) inhibits the cell cycle of breast cancer cells SUM149, promotes apoptosis, activates Caspase-3, Caspase-7, Caspase-8, Caspase-9, and increases ROS production[2].
TMI-1 (4 ng/mL, 24 h) improves the degenerative changes in the axons of 50B11 cells induced by paclitaxel (HY-B0015) and enhances the growth of neurites induced by forskolin (HY-15371), and this effect is dose-dependent[3].
TMI-1 (0.04-4 ng/mL, 24 h) reduces the expression of TRPV1 protein in 50B11 cells in a dose-dependent manner, along with a decrease in the expressions of PKC, PI3K, NF-κB, TNF-α, IL-1β, and IL-6 mRNA, as well as calcium influx[3].
In Vivo:TMI-1 (0-50 mg/kg, twice a day, 14-17 days, oral) is effective in both therapeutic and preventive arthritis mouse models, reducing disease severity[1].
TMI-1 (100 mg/kg, daily, 30 days, oral) slows down breast cancer tumor growth and prevents tumor occurrence in a breast cancer mouse model[2].
TMI-1 (100 mg/kg, daily, 4 weeks, oral) alters the lipoprotein profile that promotes atherosclerosis but does not affect the progression of early atherosclerotic lesions[4].
Analysis of pharmacokinetics in Balb/CJ mice after a single oral dose of 50 mg/kg[1]
| Route | Dose (mg/kg) | AUC (ng•h/mL) | bioavailability (%) | t1/2 (h) | Cmax (μM) |
| oral | 50 | 1484 | 39 | 1.68 | 3 |