아토시반아세테이트

아토시반아세테이트
아토시반아세테이트 구조식 이미지
카스 번호:
914453-95-5
한글명:
아토시반아세테이트
동의어(한글):
아토시반아세테이트
상품명:
Atosiban Acetate
동의어(영문):
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
분자식:
C45H71N11O14S2
포뮬러 무게:
1054.25
MOL 파일:
914453-95-5.mol

아토시반아세테이트 속성

녹는점
>165oC (dec.)
저장 조건
4°C
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨), 물(약간 용해됨)
물리적 상태
고체
물리적 상태
단단한 모양
색상
흰색에서 회백색 고체

안전

아토시반아세테이트 C화학적 특성, 용도, 생산

용도

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.

제조 방법

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.

일반 설명

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].

아토시반아세테이트 준비 용품 및 원자재

원자재

준비 용품


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