ZOTAROLIMUS

ZOTAROLIMUS 구조식 이미지
카스 번호:
221877-54-9
상품명:
ZOTAROLIMUS
동의어(영문):
ABT 578;CS-1162;A 179578;Resolute;ZOTAROLIMUS;ZotaroliMus API;Unii-H4gxr80ize;Zotarolimus, >ZotaroliMus, >90%;ZotaroliMus(ABT-578)
CBNumber:
CB21011766
분자식:
C52H79N5O12
포뮬러 무게:
966.21
MOL 파일:
221877-54-9.mol
MSDS 파일:
SDS

ZOTAROLIMUS 속성

녹는점
100-105°C
끓는 점
1016.2±75.0 °C(Predicted)
밀도
1.25
저장 조건
Hygroscopic, -20°C Freezer, Under Inert Atmosphere
용해도
DMSO, 메탄올(약간 용해됨)
물리적 상태
고체
물리적 상태
단단한 모양
산도 계수 (pKa)
10.40±0.70(Predicted)
색상
흰색에서 연한 노란색

안전

HS 번호 29349990

ZOTAROLIMUS C화학적 특성, 용도, 생산

개요

Zotarolimus is a macrocyclic lactone immunosuppressant and a derivative of rapamycin . It binds to FKBP prolyl isomerase 1A (FKBP12; IC50 = 2.57 nM) and inhibits proliferation of human peripheral blood mononuclear cells (PBMCs), rat splenocytes, and human coronary artery smooth muscle cells (IC50s = 7, 1,337, and 0.8 nM, respectively). Zotarolimus has immunosuppressive activity in a one-way mixed lymphocyte reaction using human or rat lymphocytes (IC50s = 1.2 and 1,465 nM, respectively). It also reduces symptom severity in a rat model of experimental autoimmune encephalomyelitis (EAE; ED50 = 1.17 mg/kg per day) and delays cardiac allograft rejection in rats (ED50 = 3.71 mg/kg per day). Zotarolimus inhibits neointimal formation and reduces stenosis in pig coronary arteries when applied at 10 μg/mm to stainless steel balloon expandable stents with phosphorylcholine in a model of restenosis. Formulations containing zotarolimus have been used in drug-eluting stents in the prevention of restenosis following stent placement.

화학적 성질

Pale Yellow Solid

용도

Zotarolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by preparation of the 42-triflate ester, followed by displacement with tetrazole and purification of the two isomeric products. This structural change affords a less bioavailable product, a preferred profile for some applications. Like all tacrolimus analogues, zotarolimus binds to a receptor protein (FKBP12). The complex then binds to preventing it from interacting with target proteins. Zotarolimus is extensively cited in the literature with over 200 citations.

ZOTAROLIMUS 준비 용품 및 원자재

원자재

준비 용품


ZOTAROLIMUS 공급 업체

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