1. Materials information
Names
Name | {4-[(5,6-Diphenyl-2-pyrazinyl)(isopropyl)amino]butoxy}acetic acid |
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Synonym | More Synonyms |
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MRE-269 Biological Activity
Description | MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist. |
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Related Catalog | Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor Research Areas >> Cardiovascular Disease |
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Target | IP Receptor |
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In Vitro | MRE-269 induces endothelium-independent vasodilation of rat extralobar pulmonary artery (EPA). MRE-269 or other IP receptor agonists including epoprostenol, iloprost, treprostinil and beraprost increase cAMP levels in hPASMC[1]. MRE-269 induces concentration-dependent vasodilation in LPA(+), LPA(-), and SPA(-)[3]. |
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In Vivo | The vasorelaxant effects of MRE-269 on rat small intralobar pulmonary artery (SIPA) and EPA are the same, while the other IP receptor agonists induce less vasodilation in SIPA than in EPA[1]. MRE-269 produces substantial relaxation of rat small pulmonary artery, although its effects are only significant at high concentrations of above 10 μM (pEC50, 4.98±0.22). By contrast, in rat small pulmonary veins, MRE-269 only produces minimal relaxation over the whole concentration range, with only significant relaxation occurring at the two highest doses of MRE-269 of 10 and 100 μM[2]. |
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References | [1]. Fuchikami C, et al. A comparison of vasodilation mode among selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide]), its active metabolite MRE-269 and various prostacyclin receptor agonists in rat, porcin [2]. Orie NN, et al. Differential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-269 (ACT-333679) in rat small pulmonary arteries and veins. Prostaglandins Other Lipid Mediat. 2013 Oct;106:1-7 [3]. Kuwano K, et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses |
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Chemical & Physical Properties
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 602.1±55.0 °C at 760 mmHg |
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Molecular Formula | C25H29N3O3 |
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Molecular Weight | 419.516 |
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Flash Point | 318.0±31.5 °C |
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Exact Mass | 419.220886 |
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PSA | 75.55000 |
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LogP | 5.09 |
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Vapour Pressure | 0.0±1.8 mmHg at 25°C |
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Index of Refraction | 1.588 |
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Storage condition | 2-8℃ |
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2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
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