1. Metabolic Enzyme/Protease
    Apoptosis
  2. PAI-1
    Apoptosis
  3. TM5441

TM5441 

Cat. No.: HY-101761 Purity: 98.18%
Handling Instructions

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.

For research use only. We do not sell to patients.

TM5441 Chemical Structure

TM5441 Chemical Structure

CAS No. : 1190221-43-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 136 In-stock
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2 mg USD 96 In-stock
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5 mg USD 144 In-stock
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10 mg USD 216 In-stock
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25 mg USD 456 In-stock
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50 mg USD 780 In-stock
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100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence[1][2].

IC50 & Target

IC50: 13.9~51.1 μM (Tumor cell lines)[1]

In Vitro

TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 13.9 and 51.1 μM[1].
TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441 increases apoptosis in HT1080 and HCT116 cells[1].
TM5441 induces mitochondrial depolarization[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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[1].
TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence, prolongs lifespan in klotho null mice and elicits anti-tumorigenic and anti-angiogenic activities in cancer[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

428.82

Formula

C₂₁H₁₇ClN₂O₆

CAS No.

1190221-43-2

SMILES

ClC1=CC=C(NC(COCC(NC2=CC=CC(C3=COC=C3)=C2)=O)=O)C(C(O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 300 mg/mL (699.59 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3320 mL 11.6599 mL 23.3198 mL
5 mM 0.4664 mL 2.3320 mL 4.6640 mL
10 mM 0.2332 mL 1.1660 mL 2.3320 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

TM5441TM 5441TM-5441PAI-1ApoptosisPlasminogen activator inhibitor-1Inhibitorinhibitorinhibit

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