A PAI-1 inhibitor
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Tiplaxtinin

Item No. 9000450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid
CAS Number
393105-53-8
Synonyms
  • PAI-039
  • Tiplasinin
Molecular Formula
C24H16F3NO4
Formula Weight
439.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 14 mg/ml
λmax
252, 328 nm
SMILES
O=C(C(O)=O)C1=CN(CC2=CC=CC=C2)C3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C31
InChi Code
InChI=1S/C24H16F3NO4/c25-24(26,27)32-18-9-6-16(7-10-18)17-8-11-21-19(12-17)20(22(29)23(30)31)14-28(21)13-15-4-2-1-3-5-15/h1-12,14H,13H2,(H,30,31)
InChi Key
ODXQFEWQSHNQNI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Tiplaxtinin is an inhibitor of plasminogen activator inhibitor 1 (PAI-1; IC50 = 2.7 µM for the human enzyme).1 It inhibits differentiation of human adipocytes when used at a concentration of 5 µM.2 Tiplaxtinin (5 and 20 mg/kg) reduces tumor growth and microvessel density in a T24 bladder cancer mouse xenograft model.3 It prevents carotid artery occlusion, increases the time to occlusive thrombosis, and decreases the thrombus size in a rat model of ferric chloride-induced arterial thrombosis when administered at a dose of 1 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Elokdah, H., Abou-Gharbia, M., Hennan, J.K., et al. Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: Design, synthesis, and preclinical characterization. J. Med. Chem. 47(14), 3491-3494 (2004).

    2. Crandall, D.L., Quinet, E.M., El Ayachi, S., et al. Modulation of adipose tissue development by pharmacological inhibition of PAI-1. Arterioscler. Thromb. Vasc. Biol. 26(10), 2209-2215 (2006).

    3. Gomes-Giacoia, E., Miyake, M., Goodison, S., et al. Targeting plasminogen activator inhibitor-1 inhibits angiogenesis and tumor growth in a human cancer xenograft model. Mol. Cancer Ther. 12(12), 2697-2708 (2013).

    4. Hennan, J.K., Morgan, G.A., Swillo, R.E., et al. Effect of tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. J. Thromb. Haemost. 6(9), 1558-1564 (2008).