MedKoo Cat#: 510346 | Name: Tiplaxtinin sodium

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Tiplaxtinin sodium
Tiplaxtinin sodium
CAS#Tiplaxtinin sodium

Theoretical Analysis

MedKoo Cat#: 510346

Name: Tiplaxtinin sodium

CAS#: Tiplaxtinin sodium

Chemical Formula: C24H15F3NNaO4

Exact Mass: 439.1031

Molecular Weight: 461.37

Elemental Analysis: C, 62.48; H, 3.28; F, 12.35; N, 3.04; Na, 4.98; O, 13.87

Price and Availability

Size Price Availability Quantity
Bulk Inquiry
Buy Now
Add to Cart
Synonym
Tiplaxtinin; PAI039; PAI-039; PAI 039; Tiplaxtinin sodium
IUPAC/Chemical Name
sodium 2-(1-benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)-2-oxoacetate
InChi Key
ZXKHVAUCXDHQOG-UHFFFAOYSA-M
InChi Code
InChI=1S/C24H16F3NO4.Na/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);/q;+1/p-1
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.[Na+]
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
More Info
        

Preparing Stock Solutions

The following data is based on the product molecular weight 461.37 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
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.