Treprostinil (diethanol<wbr/>amine salt)

Treprostinil (diethanolamine salt)

CAT N°: 11927
Price:

From €162.00 €137.70

Treprostinil is a derivative of prostaglandin I2 (PGI2/prostacyclin; Item No. 18220) and an agonist of PGI2, PGD2, and PGE2 receptors IP2, DP2, and EP2.{49660,49661} It binds selectively to IP2, DP2, and EP2 over EP1, EP3, and EP4 receptors with Ki values of 32, 4.4, 3.6, 212, 2,505, and 826 nM, respectively, in radioligand binding assays.{49661} Treprostinil inhibits LPS-induced production of TNF-?, IL-1?, IL-6, and granulocyte macrophage colony-stimulating factor (GM-CSF) in isolated human alveolar macrophages when used at a concentration of 200 ng/ml.{12665} It also prevents LPS-induced nuclear translocation and activation of NF-?B in the same cells. Treprostinil relaxes isolated small pulmonary arteries and veins precontracted with the thromboxane A2 (TP) receptor antagonist U-46619 (Item No. 16450), an effect that can be blocked by IP receptor antagonists in the arteries and reduced by IP receptor antagonists in the veins{49662}. It reduces right ventricular systolic pressure, but not right ventricular hypertrophy, compared to hypoxic and sham control animals in a mouse model of chronic hypoxic pulmonary hypertension.{49663} Formulations containing treprostinil have been used in the treatment of primary pulmonary hypertension.

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