TM5275 (sodium) [1103926-82-4]
Cat# HY-100447-10mg
Size : 10mg
Brand : MedChemExpress
TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
For research use only. We do not sell to patients.
TM5275 sodium Chemical Structure
CAS No. : 1103926-82-4
This product is a controlled substance and not for sale in your territory.
Based on 4 publication(s) in Google Scholar
Description |
TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM. |
IC50 & Target |
IC50: 6.95 μM (PAI-1)[1] |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
In Vitro |
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[1]. 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[2]. 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[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
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)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Molecular Weight |
543.97 |
||||||||||||
Formula |
C28H27ClN3NaO5 |
||||||||||||
CAS No. |
1103926-82-4 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
White to off-white |
||||||||||||
SMILES |
O=C(O[Na])C1=CC(Cl)=CC=C1NC(COCC(N2CCN(C(C3=CC=CC=C3)C4=CC=CC=C4)CC2)=O)=O |
||||||||||||
Shipping | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Storage |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
||||||||||||
Solvent & Solubility |
In Vitro:
DMSO : 62.5 mg/mL (114.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
|
||||||||||||
Purity & Documentation |
Purity: 98.99% |
||||||||||||
References |
|
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 1.8383 mL | 9.1917 mL | 18.3834 mL | 45.9584 mL |
5 mM | 0.3677 mL | 1.8383 mL | 3.6767 mL | 9.1917 mL | |
10 mM | 0.1838 mL | 0.9192 mL | 1.8383 mL | 4.5958 mL | |
15 mM | 0.1226 mL | 0.6128 mL | 1.2256 mL | 3.0639 mL | |
20 mM | 0.0919 mL | 0.4596 mL | 0.9192 mL | 2.2979 mL | |
25 mM | 0.0735 mL | 0.3677 mL | 0.7353 mL | 1.8383 mL | |
30 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.5319 mL | |
40 mM | 0.0460 mL | 0.2298 mL | 0.4596 mL | 1.1490 mL | |
50 mM | 0.0368 mL | 0.1838 mL | 0.3677 mL | 0.9192 mL | |
60 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7660 mL | |
80 mM | 0.0230 mL | 0.1149 mL | 0.2298 mL | 0.5745 mL | |
100 mM | 0.0184 mL | 0.0919 mL | 0.1838 mL | 0.4596 mL |
TM5275 sodium Related Classifications
- Metabolic Enzyme/Protease
- PAI-1