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NS-304

NS-304
NS-304 structure
CAS No.
475086-01-2
Chemical Name:
NS-304
Synonyms
NS-304;Slipper;elexipag;Selexipag;ACT-293987;Selexipag API;NS-304(Selexipag);Selexipag(NS-304);NS-304;ACT-293987;Selexipag intermediate 1
CBNumber:
CB32454222
Molecular Formula:
C26H32N4O4S
Formula Weight:
496.62
MOL File:
475086-01-2.mol

NS-304 Properties

Density 
1.210±0.06 g/cm3(Predicted)
pka
3.82±0.40(Predicted)
FDA UNII
5EXC0E384L
ATC code
B01AC27

NS-304 price More Price(23)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 10010411 NS-304 ≥98% 475086-01-2 1mg $36 2021-12-16 Buy
Cayman Chemical 10010411 NS-304 ≥98% 475086-01-2 5mg $162 2021-12-16 Buy
Tocris 3351 Selexipag ≥98%(HPLC) 475086-01-2 10 $254 2021-12-16 Buy
Tocris 3351 Selexipag ≥98%(HPLC) 475086-01-2 50 $1072 2021-12-16 Buy
TRC S253150 Selexipag 475086-01-2 50mg $340 2021-12-16 Buy

NS-304 Chemical Properties,Uses,Production

Description

Selexipag and its active metabolite, the corresponding carboxylic acid, are nonprostanoid prostaglandin I2 (PGI-2) receptor agonists. The N-methylsulfonamide within selexipag is hydrolyzed to the corresponding carboxylic acid in vivo by hepatic microsomes at a rate which provides a slow-release pharmacological effect. The compound was originally discovered by Nippon Shinyaki and later licensed to Actelion for development. The drug was approved in 2015 and first launched for the oral treatment of pulmonary arterial hypertension (PAH) in the U.S. in 2016 to delay disease progression and reduce the risk of hospitalization.

Description

Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells and platelets. The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation. NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.

Uses

Selexipag is an orally available, highly selective, long-acting prostacyclin (IP) receptor agonist prodrug. It is a potential drug for the treatment of various vascular disorders such as pulmonary arterial hypertension and arteriosclerosis obliterans.

Definition

ChEBI: A member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the tre tment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid).

Chemical Synthesis

The synthesis of selexipag began with condensation of commercially available benzil (51) and glycinamide hydrochloride in the presence of concentrated sodium hydroxide in refluxing MeOH to yield hydroxypyrazine 52. This compound was subsequently converted to 5-chloro-2,3-diphenylpyrazine (53) upon treatment with refluxing POCl3 in the presence of a catalytic amount of H2SO4. Chloride 53 was then subjected to neat 4-(isopropylamino)-1-butanol (54, prepared by the reductive alkylation of 4-amino-1-butanol and acetone with hydrogen over PtO2 in EtOH) at 190 °C to give aminopyrazinyl alcohol 55 in 56% yield as colorless crystals. Alcohol 55 was alkylated with tert-butyl bromoacetate using Bu4NHSO4 as a phase-transfer catalyst and 40% aqueous KOH in benzene to give ester 56. Although it is particularly unusual to employ benzene on a production scale, these are the only reported conditions for this transformation. The crude ester 56 was then saponified using methanolic sodium hydroxide to yield the corresponding carboxylic acid 57 in 62% as pale-yellow crystals in two steps from compound 55. Finally, the carboxylic acid 57 was coupled with methanesulfonamide in the presence of CDI and DBU in THF to give selexipag (VI) in 77% yield.

NS-304 Preparation Products And Raw materials

Raw materials

Preparation Products


NS-304 Suppliers

Global( 156)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 15426 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 9115 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29954 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
Shenzhen Excellent Biotech Co., Ltd.
13480692018
ramyan@ex-biotech.com;sale@ex-biotech.com CHINA 955 58
Zhuozhou Wenxi import and Export Co., Ltd
+8613111626072 (WhatsApp)
Wechat: +8613111626072 Wickr me: waynehu zzwenxi@126.com CHINA 13187 58

View Lastest Price from NS-304 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-12-01 Selexipag
475086-01-2
US $10.00 / Kg/Drum 1KG 98% 10 ton Hebei Crovell Biotech Co Ltd
2021-09-29 selexipag
475086-01-2
US $0.00 / KG 10g 99%min 10kg WUHAN FORTUNA CHEMICAL CO., LTD
2021-07-13 Selexipag
475086-01-2
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

475086-01-2(NS-304)Related Search:


  • NS-304
  • Selexipag
  • ACT-293987
  • NS-304(Selexipag)
  • Selexipag API
  • 2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylaMino]butoxy]-N-MethylsulfonylacetaMide
  • AcetaMide, 2-[4-[(5,6-diphenyl-2-pyrazinyl)(1-Methylethyl)aMino]butoxy]-N- (Methylsulfonyl)-
  • Slipper
  • Selexipag intermediate 1
  • 2-[4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide
  • 2-[4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamine]butyloxy]-N-(methylsulfonyl)acetamide
  • Selexipag intermediate 2
  • Selexipag(NS-304)
  • NS-304;ACT-293987
  • 2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-N-(methylsulfonyl)acetamide
  • SELEXIPAG;ACT293987;NS304;NS 304;ACT 293987;ACT-293987
  • (2R,3R,4R,5R)-2,3,4,5,6-pentahydroxyhexyl2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetate
  • Selexipag 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-N-(methylsulfonyl)acetamide
  • Selexipag (10mM in DMSO)
  • elexipag
  • 475086-01-2
  • 1475086-75-0
  • 242042-71-7
  • 75086-01-2
  • non-prostanoid prostacyclin (PGI2) receptor agonist
  • Selexipag
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