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HomeProduct name list[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID Structural

What is [4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID?

Description

Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets. The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation. MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs. Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor. As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.

The Uses of [4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

MRE-269 an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269 is used for the treatment of pulmonary arterial hypertension. MRE-269 is an active metabolite of Selexipag (S253150).

Definition

ChEBI: A member of the class of pyrazines that is {4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetic acid carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. The active metabolite of selexipag, an orphan drug used for the treatm nt of pulmonary arterial hypertension.

Properties of [4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

Melting point: 116 - 118°C
Boiling point: 602.1±55.0 °C(Predicted)
Density  1.160
storage temp.  Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility  Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form  Solid
pka 3.51±0.10(Predicted)
color  Off-White to Light Yellow

Safety information for [4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for [4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

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