Tiplaxtinin (PAI-039)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1020 | Check With Us |
| 500mg | $1550 | Check With Us |
| 1g | $2325 | Check With Us |
: Cat #: V1883 CAS #: 393105-53-8 Purity ≥ 98%
Description: Tiplaxtinin(PAI-039) is an orally bioactive and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 μM.
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| Molecular Weight (MW) | 439.38 |
|---|---|
| Molecular Formula | C24H16F3NO4 |
| CAS No. | 393105-53-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 72 mg/mL (163.9 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 18 mg/mL (41 mM) | |
| Solubility In Vivo | 2.0% Tween 80+0.5% methylcellulose: 30mg/mL |
| SMILES Code | O=C(O)C(C1=CN(CC2=CC=CC=C2)C3=C1C=C(C4=CC=C(OC(F)(F)F)C=C4)C=C3)=O |
| Synonyms | PAI039; PAI-039; PAI 039. |
| Protocol | 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 IC50 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 IC50 value of 70.3±0.1 μM. Notably, IC50 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 IC50 values calculated for cells cultured in the presence of Tiplaxtinin under attached conditions. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2759 mL | 11.3797 mL | 22.7593 mL | 45.5187 mL |
| 5mM | 0.4552 mL | 2.2759 mL | 4.5519 mL | 9.1037 mL |
| 10mM | 0.2276 mL | 1.1380 mL | 2.2759 mL | 4.5519 mL |
| 20mM | 0.1138 mL | 0.5690 mL | 1.1380 mL | 2.2759 mL |
The molarity calculator equation
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The dilution calculator equation
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.