Tiplaxtinin
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MedKoo CAT#: 510346

CAS#: 393105-53-8

Description: Tiplaxtinin, also known as PAI-039, is a novel plasminogen activator inhibitor-1 (PAI-1) inhibitor. The pharmacokinetic profile of PAI-039 indicated an oral bioavailability of 43 +/- 15.3% and a plasma half-life of 6.2 +/- 1.3 h. PAI-039 is an orally active prothrombolytic drug that inhibits PAI-1 and accelerates fibrinolysis while maintaining normal coagulation in a model of coronary occlusion . PAI-039 exerts antithrombotic efficacy in rat models of arterial and venous vascular injury without effecting platelet aggregation. PAI-039 as a novel therapeutic may improve diabetic wound closure.


Chemical Structure

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Tiplaxtinin
CAS# 393105-53-8

Theoretical Analysis

MedKoo Cat#: 510346
Name: Tiplaxtinin
CAS#: 393105-53-8
Chemical Formula: C24H16F3NO4
Exact Mass: 439.10314
Molecular Weight: 439.38
Elemental Analysis: C, 65.60; H, 3.67; F, 12.97; N, 3.19; O, 14.57

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 2 Weeks
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 950.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2850.0 2 Weeks
2.0g USD 3850.0 2 Weeks
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Synonym: Tiplaxtinin; PAI039; PAI-039; PAI 039.

IUPAC/Chemical Name: 2-(1-benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)-2-oxoacetic acid

InChi Key: ODXQFEWQSHNQNI-UHFFFAOYSA-N

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)

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 439.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Rebalka IA, Raleigh MJ, D'Souza DM, Coleman SK, Rebalka AN, Hawke TJ. Inhibition of PAI-1 via PAI-039 improves dermal wound closure in diabetes mellitus. Diabetes. 2015 Mar 9. pii: db141174. [Epub ahead of print] PubMed PMID: 25754958.

2: Hennan JK, Morgan GA, Swillo RE, Antrilli TM, Mugford C, Vlasuk GP, Gardell SJ, Crandall DL. Effect of tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. J Thromb Haemost. 2008 Sep;6(9):1558-64. doi: 10.1111/j.1538-7836.2008.03063.x. Epub 2008 Jul 4. PubMed PMID: 18624980.

3: Hennan JK, Elokdah H, Leal M, Ji A, Friedrichs GS, Morgan GA, Swillo RE, Antrilli TM, Hreha A, Crandall DL. Evaluation of PAI-039 [{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid], a novel plasminogen activator inhibitor-1 inhibitor, in a canine model of coronary artery thrombosis. J Pharmacol Exp Ther. 2005 Aug;314(2):710-6. Epub 2005 Apr 28. PubMed PMID: 15860572.

 



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