475085-57-5 Usage
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.
Uses
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.
Check Digit Verification of cas no
The CAS Registry Mumber 475085-57-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,7,5,0,8 and 5 respectively; the second part has 2 digits, 5 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 475085-57:
(8*4)+(7*7)+(6*5)+(5*0)+(4*8)+(3*5)+(2*5)+(1*7)=175
175 % 10 = 5
So 475085-57-5 is a valid CAS Registry Number.
475085-57-5Relevant articles and documents
Synthesis method of diphenyl pyrazine derivative
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, (2021/06/13)
The invention discloses a synthesis method of a diphenyl pyrazine derivative. The method is characterized in that benzil and glycinamide are used as raw materials, and a target product is prepared through five-step reaction. The obtained target product is high in purity, subsequent production of high-quality drugs is facilitated, and the synthesis method is reasonable in route design, mild in reaction condition, free of high-temperature reaction, good in safety and high in feasibility.
CRYSTAL
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Paragraph 0094, (2020/08/12)
A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as “Compound B”). A form-I crystal of Compound B, which shows peaks at diffraction an
POLYMORPHIC FORMS AND AMORPHOUS SOLID DISPERSION OF SELEXIPAG
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, (2018/02/28)
The present disclosure relates to crystalline forms of selexipag and their processes for preparation. The present disclosure also relates to an amorphous solid dispersion of selexipag and its processes for their preparation as well as premix of crystalline selexipag and their process.
