store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 79.00 | |
10 mg | In stock | $ 122.00 | |
25 mg | In stock | $ 263.00 | |
50 mg | In stock | $ 493.00 | |
100 mg | In stock | $ 701.00 | |
500 mg | In stock | $ 1,460.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 88.00 |
Description | TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1). |
Targets&IC50 | Tumor cell lines:9.7~60.3 μM |
In vitro | 1.TM5441 inhibits branching of human umbilical vein endothelial cells (HUVECs) in a vasculature assay in vitro when used at a concentration of 50 μM but does not affect HUVEC survival or apoptosis. 2.TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 9.7 and 60.3 μM. TM5441 decreases tumor cell viability in part through diminished proliferation. TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441is a potent stimulators of intrinsic apoptosis in tumor cells. TM5441 induces mitochondrial depolarization. In mouse proximal tubular epithelial cells, TM5441 effectively inhibits PAI-1-induced mRNA expression of fibrosis and inflammation markers and also reverses PAI-1-induced inhibition of plasmin activity |
In vivo | 1.It also disrupts tumor vasculature in HT1080 and HCT116 mouse xenograft models when used at a dose of 20 mg/kg per day. TM5441 prevents hypertension and cardiac hypertrophy and reduces periaortic fibrosis induced by L-NAME . It protects against high-fat diet-induced non-alcoholic fatty liver disease (NAFLD) in mice when administered concurrently with a high-fat diet or after glucose tolerance has developed. TM5441 also increases median lifespan by 4-fold and reduces signs of senescence in Klotho-deficient mice, a mouse model of aging.2.Oral administration of TM5441 (20 mg/kg daily) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival. The average peak plasma concentration is 11.4 μM one hour after oral administration and undetectable levels 23 hours after administration. TM5441 effectively inhibits albuminuria, mesangial expansion, ECM accumulation, and macrophage infiltration in diabetic kidneys |
Kinase Assay | TM5441 is dissolved with DMSO at a stock concentration of 50 mM.HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells are treated with 0-100 μM TM5441 for 48 hours at 37°C. Cell viability is measured by MTT assay. |
Animal Research | TM5441 is prepared in 0.5% carboxymethyl cellulose.Mice: TM5275 at 50 mg/kg/day and TM5441 at 10 mg/kg/day were orally administered in control and diabetic mice for 16 weeks. Mice were monitored at least once a day. At the end, blood is collected for measurement of plasma glucose and creatinine, urine for protein measurement, and kidneys for immunohistochemical analysis. |
Molecular Weight | 428.82 |
Formula | C21H17ClN2O6 |
CAS No. | 1190221-43-2 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 300 mg/mL
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TM5441 1190221-43-2 Apoptosis Metabolism PAI-1 Plasminogen activator inhibitor-1 Inhibitor TM 5441 TM-5441 inhibit inhibitor