[CAS NO. 393105-53-8]  Tiplaxtinin

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PRODUCTS SPECIFICATIONS [393105-53-8]

Catalog
HY-15253
Brand
MCE
CAS
393105-53-8

DESCRIPTION [393105-53-8]

Overview

MDLMFCD09475615
Molecular Weight439.38
Molecular FormulaC24H16F3NO4
SMILESO=C(C(O)=O)C1=CN(CC2=CC=CC=C2)C(C1=C3)=CC=C3C4=CC=C(OC(F)(F)F)C=C4

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


Summary

Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 ( PAI-1 ) with IC 50 of 2.7 μM [1] .


IC50 & Target

IC50: 2.7 μM (PAI-1) [1]


In Vitro

Tiplaxtinin (PAI-039), a small-molecule inhibitor of PAI-1 activity, on the urothelial cell lines. A significant inhibition in cellular proliferation is noted in T24 cells treated with Tiplaxtinin with the documentation of a favorable IC 50 value of 43.7±6.3 μM and in UM-UC-14 cells 52.8±1.6 μM whereas the benign cell line, UROtsa, is noted to have a higher IC 50 value of 70.3±0.1 μM. Notably, IC 50 values of Tiplaxtinin in detached cells, 19.7±3.8 μM in T24, 44.5±6.5 μM in UM-UC-14, and 31.6±6.1 μM in UROtsa, are significantly lower than the IC 50 values calculated for cells cultured in the presence of Tiplaxtinin under attached conditions [2] .

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


In Vivo

In the vena cava protocol, Tiplaxtinin (PAI-039) pretreatment significantly reduces thrombus weight at Tiplaxtinin doses of 3, 10 and 30 mg/kg. When Tiplaxtinin is dosed in a treatment paradigm 4 h after stable arterial and venous thrombosis, a significant reduction in thrombus weight is observed 24 h later at Tiplaxtinin doses of 3, 10 and 30 mg/kg [1] . Tiplaxtinin (PAI-039) is administered by oral gavage to athymic mice bearing human bladder cancer cell line T24 xenografts and human cervical cancer HeLa cell xenografts. The subcutaneous tumor growth of both T24 and HeLa cell xenografts treated with Tiplaxtinin is markedly reduced compared with untreated controls. Specifically, at the end of the study, control T24 xenografts are noted to be 1,150±302 mm 3 compared with 593±328 mm 3 for T24 xenograft tumors treated with 5 mg/kg Tiplaxtinin (P<0.0001) and 627±248 mm 3 for T24 xenografts treated with 20 mg/kg (P<0.0001) [2] . Tiplaxtinin (1, 3, and 10 mg/kg) is subjected to electrolytic injury of the coronary artery. Tiplaxtinin (PAI-039) causes prolongation in time to coronary occlusion (control, 31.7±6.3 min; 3 mg/kg Tiplaxtinin, 66.0±6.4 min; 10 mg/kg, 56.7±7.4 min; n=5-6; p<0.05) and a reduced thrombus weight (control, 7.6±1.5 mg; 10 mg/kg Tiplaxtinin, 3.6±1.0 mg; p<0.05) [3] .

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


Appearance

Solid


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 : 100 mg/mL ( 227.59 mM ; Need ultrasonic)

H 2 O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2759 mL 11.3797 mL 22.7593 mL
5 mM 0.4552 mL 2.2759 mL 4.5519 mL
10 mM 0.2276 mL 1.1380 mL 2.2759 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 (5.69 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.69 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

1H-Indole-3-acetic acid, α-oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-
α-Oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid
PAI 039
Tiplaxtinin
Tiplasinin