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Treprostinil

Cat. No. M7428
Treprostinil Structure
Synonym:

UT-15; LRX-15

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 290  USD290 In stock
50mg USD 430  USD430 In stock
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Quality Control & Documentation
Biological Activity

Treprostinil (UT-15) is a potent prostacyclin (PGI2) analog (EC50 values are 0.6, 1.9 and 6.2 nM at DP1, IP and EP2 receptors respectively). Causes vasodilation of human pulmonary arteries and inhibits NFκB nuclear translocation in human alveolar macrophages in vitro.

Chemical Information
Molecular Weight 390.51
Formula C23H34O5
CAS Number 81846-19-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David M Smadja, et al. Thromb Haemost . Treprostinil indirectly regulates endothelial colony forming cell angiogenic properties by increasing VEGF-A produced by mesenchymal stem cells

[2] Brendan J Whittle, et al. Biochem Pharmacol . Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist

[3] N Ghonem, et al. Am J Transplant . Treprostinil, a prostacyclin analog, ameliorates ischemia-reperfusion injury in rat orthotopic liver transplantation

[4] V S Nikam, et al. Eur Respir J . Treprostinil inhibits the recruitment of bone marrow-derived circulating fibrocytes in chronic hypoxic pulmonary hypertension

[5] Ghoshal and Jacob. Biochem Pharmacol. An alternative molecular mechanism of action of 5-fluorouracil, a potent anticancer drug.

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Keywords: Treprostinil, UT-15; LRX-15 supplier, Prostaglandin Receptor, inhibitors, activators

 
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