Treprostinil (diethanolamine salt) – 5 mg

Brand:
Cayman
CAS:
830354-48-8
Storage:
-20
UN-No:
Non-Hazardous - /

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-α, IL-1β, 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-κB 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.  

 

Available on backorder

SKU: 11927 - 5 mg Category:

Description

An agonist of IP2, DP2, and EP2 receptors; binds selectively to IP2, DP2, and EP2 over EP1, EP3, and EP4 receptors (Kis = 32, 4.4, 3.6, 212, 2,505, and 826 nM, respectively, in radioligand binding assays); inhibits LPS-induced production of TNF-α, IL-1β, IL-6, and GM-CSF in in isolated human alveolar macrophages at 200 ng/ml; relaxes isolated small pulmonary arteries and veins precontracted with U-46619; reduces right ventricular systolic pressure compared to hypoxic and sham control animals in a mouse model of chronic hypoxic pulmonary hypertension


Formal name: 2-[[(1R,2R,3aS,9aS)-2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]oxy]-acetic acid, diethanolamine salt

Synonyms:  Treprostinil diolamine|UT 15C

Molecular weight: 495.7

CAS: 830354-48-8

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Lipids|Prostaglandins||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway