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Atosiban Acetate

Atosiban Acetate Struktur
914453-95-5
CAS-Nr.
914453-95-5
Englisch Name:
Atosiban Acetate
Synonyma:
Atosiban Acetate(acetate);Atosiban acetate (90779-69-4 free base);1-{[7-(2-Amino-2-oxoethyl)-13-sec-butyl-16-(4-ethoxybenzyl)-10-(1 -hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pent aazacycloicosan-4-yl]carbonyl}prolylornithylglycinamide acetate ( 1:1);nonapeptide,Preterm,vasopressin,Atosiban,RWJ-22164,tocolytic,RW-22164,desamino-oxytocin,inhibit,Ca2+,Vasopressin Receptor,RW 22164,oxytocin,maternal-fetal,Atosiban acetate,RWJ 22164,Inhibitor,Oxytocin Receptor,OXTR;(2S)-N-((S)-5-amino-1-((2-amino-2-oxoethyl)amino)-1-oxopentan-2-yl)-1-((4R,7S,10S,16R)-7-(2-amino-2-oxoethyl)-13-((S)-sec-butyl)-16-(4-ethoxybenzyl)-10-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)pyrrolidine-2-carboxamide acetate;(S)-N-((S)-5-Amino-1-((2-amino-2-oxoethyl)amino)-1-oxopentan-2-yl)-1-((4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-((S)-sec-butyl)-16-(4-ethoxybenzyl)-10-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)pyrrolidine-2-carboxamide acetate;(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
CBNumber:
CB12551640
Summenformel:
C45H71N11O14S2
Molgewicht:
1054.25
MOL-Datei:
914453-95-5.mol

Atosiban Acetate Eigenschaften

Schmelzpunkt:
>165oC (dec.)
storage temp. 
4°C
L?slichkeit
DMSO (Slightly), Methanol (Slightly), Water (Slightly)
Aggregatzustand
solid
Farbe
White to Off-White Solid

Sicherheit

Atosiban Acetate Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Atosiban acetate is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research. As an oxytocin receptor blocker, it has demonstrated significant therapeutic effectiveness in the treatment of experimental endometriosis.

synthetische

Atosiban acetate(914453-95-5) is synthesized through a process called solid-phase peptide synthesis. The Solid phase peptide synthesis of atosiban involves coupling of the amino acid components in sequential manner.The first amino acid is selectively bound to a polymer resin. The amino group is then selectively de-blocked and condensed with the next amino acid. This completed one cycle is then repeated sequentially for coupling of remaining 8 protected amino acids. The protected atosiban is cleaved and de-protected to obtain crude active substance. This crude product is finally purified and the pure product obtained from HPLC purification is desalted and freeze dried to yield pure atosiban acetate.

Allgemeine Beschreibung

Atosibana is a mixed antagonist of oxytocin and vasopressin receptors [1].
Atosibana is a peptide and is a dual antagonist of oxytocin receptor (OTR) and vasopressin receptors (V1aR, V1bR, V2R). When acted as an OTR antagonist, atosibana showed pKi values of 7.9 and 7.2 for human OTR and rat OTR, respectively. Treatment of atosibana significantly inhibited cell growth in MDCK and HEK293 cells stably transfected with the human OTR with IC50 values of 15.4 nM and 20.8 nM, respectively. When acted as a vasopressin receptor antagonist, atosibana exerted pKi values of 9.8, 7.4 and 6.5 for hV1aR, hV1bR and hV2R, respectively. Atosibana has been shown to have efficacy in inhibiting uterine contractions and delaying preterm delivery. However, atosibana can not be used for long-term maintenance treatment since it is not orally bioavailable [1].

Atosiban Acetate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Atosiban Acetate Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

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914453-95-5()Verwandte Suche:


  • 1-{[7-(2-Amino-2-oxoethyl)-13-sec-butyl-16-(4-ethoxybenzyl)-10-(1 -hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pent aazacycloicosan-4-yl]carbonyl}prolylornithylglycinamide acetate ( 1:1)
  • (2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
  • (2S)-N-((S)-5-amino-1-((2-amino-2-oxoethyl)amino)-1-oxopentan-2-yl)-1-((4R,7S,10S,16R)-7-(2-amino-2-oxoethyl)-13-((S)-sec-butyl)-16-(4-ethoxybenzyl)-10-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)pyrrolidine-2-carboxamide acetate
  • Atosiban acetate (90779-69-4 free base)
  • Atosiban Acetate(acetate)
  • nonapeptide,Preterm,vasopressin,Atosiban,RWJ-22164,tocolytic,RW-22164,desamino-oxytocin,inhibit,Ca2+,Vasopressin Receptor,RW 22164,oxytocin,maternal-fetal,Atosiban acetate,RWJ 22164,Inhibitor,Oxytocin Receptor,OXTR
  • (S)-N-((S)-5-Amino-1-((2-amino-2-oxoethyl)amino)-1-oxopentan-2-yl)-1-((4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-((S)-sec-butyl)-16-(4-ethoxybenzyl)-10-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)pyrrolidine-2-carboxamide acetate
  • 914453-95-5
  • C43H67N11O12S2C2H4O
  • Amines, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals
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