CS-2524
TM5275 (sodium)
CAS: 1103926-82-4
Molecular Formula: C28H29ClN3NaO5
CS-2524 - Names and Identifiers
CS-2524 - Physico-chemical Properties
| Molecular Formula | C28H29ClN3NaO5 |
| Molar Mass | 546 |
| Solubility | DMSO: ≥100 mg/mL |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| In vitro study | Docking studies shows that TM5275 binds to strand 4 of the A β-sheet (s4A) position of PAI-1. TM5275 is a selective PAI-1 and (up to 100 μM) does not interfere with other serpin/serine protease systems. TM5275 at concentrations of 20 and 100 μM significantly prolongs the retention of tPA-GFP on VECs by inhibiting tPA-GFP-PAI-1 high-molecular-weight complex formation. TM5275 enhances the time-dependent accumulation of plasminogen as well as the dissolution of fibrin clots on and around the tPA-GFP-expressing cells. Cell viability at 72 h treatment is decreased with 70-100 μM TM5275 in ES-2 and JHOC-9 cells. From 48 h up to 96 h, cell growth is suppressed with 100 μM TM5275. Active PAI-1 in cell culture media is significantly decreased in cells treated with 100 μM TM5275 compared to control treatment. TM5275 is suggested to exert anti-proliferative effects in ovarian cancer with high PAI-1 expression. |
| In vivo study | TM5275 exhibits a favorable pharmacokinetics profile and very low toxicity to mice and rats. In rat thrombosis models. Blood clot weights are significantly lower in rats administered 10 and 50 mg/kg of TM5275 (60.9±3.0 and 56.8±2.8 mg, respectively) than in vehicle-treated rats (72.5±2.0 mg). The antithrombotic effectiveness of TM5275 (50 mg/kg) is equivalent to that of ticlopidine (500 mg/kg), a reference antithrombotic compound. Plasma concentration of TM5275 reaches 17.5±5.2 μM after a dose of 10 mg/kg. TM5275 (5 mg/kg) combined with tPA (0.3 mg/kg) significantly enhances the antithrombotic effect of tPA (0.3 mg/kg) alone and provides a benefit similar to that of a high tPA dose (3 mg/kg). |
CS-2524 - Risk and Safety
| UN IDs | UN 3077 9 / PGIII |
CS-2524 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.835 ml | 9.175 ml | 18.349 ml |
| 5 mM | 0.367 ml | 1.835 ml | 3.67 ml |
| 10 mM | 0.183 ml | 0.917 ml | 1.835 ml |
| 5 mM | 0.037 ml | 0.183 ml | 0.367 ml |
Last Update：2024-01-02 23:10:35
CS-2524 - Reference Information
| bioactivity | TM 5275 sodium is an oral, bioactive plasmin activator inhibitor-1 (PAI-1) the IC50 value of the inhibitor is 6.95 μm. |
| Target | Value |
| PAI-1 (Cell-free assay) | 6.95 μM |
Last Update：2024-04-09 15:16:56
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Spot supply
Product Name: TM5275 (sodium) Visit Supplier Webpage Request for quotationCAS: 1103926-82-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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