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ZOTAROLIMUS

ZOTAROLIMUS Structure
CAS No.
221877-54-9
Chemical Name:
ZOTAROLIMUS
Synonyms
ABT 578;CS-1162;A 179578;Resolute;ZOTAROLIMUS;ZotaroliMus API;Unii-H4gxr80ize;Zotarolimus, >ZotaroliMus, >90%;ZotaroliMus(ABT-578)
CBNumber:
CB21011766
Molecular Formula:
C52H79N5O12
Molecular Weight:
966.21
MOL File:
221877-54-9.mol
MSDS File:
SDS
Modify Date:
2023/5/18 11:30:58

ZOTAROLIMUS Properties

Melting point 100-105°C
Boiling point 1016.2±75.0 °C(Predicted)
Density 1.25
storage temp. Hygroscopic, -20°C Freezer, Under Inert Atmosphere
solubility DMSO, Methanol (Slightly)
form Solid
pka 10.40±0.70(Predicted)
color White to Pale Yellow

SAFETY

Risk and Safety Statements

HS Code  29349990

ZOTAROLIMUS Chemical Properties,Uses,Production

Description

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.

Chemical Properties

Pale Yellow Solid

Uses

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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TargetMol Chemicals Inc. +1-781-999-5354 United States 19973 58 Inquiry

ZOTAROLIMUS Spectrum

ZOTAROLIMUS (42S)-42-Deoxy-42-(1H-tetrazol-1-yl)rapamycin A 179578 ABT 578 Rapamycin, 42-deoxy-42-(1H-tetrazol-1-yl)-, (42S)- Unii-H4gxr80ize ZotaroliMus, >90% 42-(1-Tetrazolyl)rapamycin Resolute ZotaroliMus API 42-deoxy-42-(1H-tetrazol-1-yl)-(42S)-Rapamycin (42S)-42-Deoxy-42-(1H-tetrazol-1-yl)rapamycin Zotarolimus(ABT-578) A 179578 Resolute Zotarolimus A 179578 ZotaroliMus(ABT-578) ABT-578;A-179578;ABT578;A179578;ABT 578;A 179578 CS-1162 Zotarolimus, > ZOTAROLIMUS USP/EP/BP ZOTAROLIMUS Impurities 221877-54-9 C52H79N5O12 Inhibitors Chiral Reagents Heterocycles Intermediates & Fine Chemicals Pharmaceuticals