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ZOTAROLIMUS

Product Name
ZOTAROLIMUS
CAS No.
221877-54-9
Chemical Name
ZOTAROLIMUS
Synonyms
CS-1162;ABT 578;Resolute;A 179578;ZOTAROLIMUS;Unii-H4gxr80ize;ZotaroliMus API;Zotarolimus, >ZotaroliMus, >90%;ZotaroliMus(ABT-578)
CBNumber
CB21011766
Molecular Formula
C52H79N5O12
Formula Weight
966.21
MOL File
221877-54-9.mol
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ZOTAROLIMUS Property

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
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Safety

HS Code 
29349990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
29246
Product name
Zotarolimus
Packaging
5mg
Price
$93
Updated
2024/03/01
Cayman Chemical
Product number
29246
Product name
Zotarolimus
Packaging
25mg
Price
$343
Updated
2024/03/01
Cayman Chemical
Product number
29246
Product name
Zotarolimus
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
29246
Product name
Zotarolimus
Packaging
10mg
Price
$169
Updated
2024/03/01
TRC
Product number
Z700800
Product name
Zotarolimus,>90%
Packaging
10mg
Price
$145
Updated
2021/12/16
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ZOTAROLIMUS Chemical Properties,Usage,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.

Uses

A tetrazole-containing Rapamycin analog as immunomodulator and useful in the treatment of restenosis and immune and autoimmune diseases.

Definition

ChEBI: Zotarolimus is a macrolide and a lactam.

in vivo

Zotarolimus (0.1-10 mg/kg; oral administration; on days 1, 4, 5, 6, and 7) inhibits the rat adjuvant-induced delayed-type hypersensitivity (DTH) response in a dose-dependent manner with an?ED50?value of 1.72 mg/kg/day in the rat adjuvant DTH model[1].
Zotarolimus (0.1-10 mg/kg; oral administration; once daily; for 13 days) inhibits the rat experimental autoimmune encephalomyelitis (EAE) in a dose - dependent manner with an?ED50?value of 1.17 mg/kg/day in the rat EAE model[1].
Zotarolimus (0.1-10 mg/kg; oral administration; once daily; for 13 days) shows a dose-related delay in cardiac allograft rejection with an?ED50?value of 3.71 mg/kg/day in the rat cardiac allograft rejection model[1].

Animal Model:Male Sprague-Dawley rats (about 130 g) induced delayed-type hypersensitivity (DTH) model[1].
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg (10% ethanol, 40% propylene glycol, and 50% of a mixture of 4% cremophor EL in D5W (EPC))
Administration:Oral administration, on days 1, 4, 5, 6, and 7
Result:Inhibited the rat adjuvant-induced DTH response in a dose-dependent manner.
Animal Model:Male Lewis rats (about 220 g) bearing autoimmune encephalomyelitis (EAE)[1].
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
Administration:Oral administration, once daily, for 13 days
Result:Inhibited the rat EAE in a dose-dependent manner.
Animal Model:Lewis rats bearing heterotopic ear-heart transplant[1].
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
Administration:Oral administration, once daily, for 13 days
Result:Caused a dose-related delay in cardiac allograft rejection.

References

[1] ROBIN COLLINGWOOD. Stent-based delivery of ABT-578 via a phosphorylcholine surface coating reduces neointimal formation in the porcine coronary model[J]. Catheterization and Cardiovascular Interventions, 2005, 65 2: 227-232. DOI: 10.1002/ccd.20348
[2] YUNG-WU CHEN. Zotarolimus, a novel sirolimus analogue with potent anti-proliferative activity on coronary smooth muscle cells and reduced potential for systemic immunosuppression.[J]. Journal of Cardiovascular Pharmacology, 2007, 49 4: 228-235. DOI: 10.1097/fjc.0b013e3180325b0a

ZOTAROLIMUS Preparation Products And Raw materials

Raw materials

Preparation Products

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ZOTAROLIMUS Suppliers

Canada 1 China 115 India 2 South Korea 1 United Kingdom 3 United States 20 Global 142
J & K SCIENTIFIC LTD.
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18210857532; 18210857532
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86-10-82849933
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jkinfo@jkchemical.com
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Chembest Research Laboratories Limited
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+86-21-20908456
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021-58180499
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sales@BioChemBest.com
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LGM Pharma
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1-(800)-881-8210
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615-250-9817
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inquiries@lgmpharma.com
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United States
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Chemsky（shanghai）International Co.,Ltd.
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021-50135380
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shchemsky@sina.com
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China
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32321
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
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China
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Nanjing Sunlida Biological Technology Co., Ltd.
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025-57798810
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025-57019371
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sales@sunlidabio.com
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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Jinan Mingya Medical Technology Co., Ltd.
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0531-85828981
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+86-531-85806006
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864598798@qq.com
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China
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
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HBCChem, Inc.
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221877-54-9, ZOTAROLIMUSRelated Search:

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  • ZOTAROLIMUS
  • (42S)-42-Deoxy-42-(1H-tetrazol-1-yl)rapamycin
  • A 179578
  • ABT 578
  • ABT-578;A-179578;ABT578;A179578;ABT 578;A 179578
  • CS-1162
  • 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)
  • Zotarolimus, &gt
  • ZOTAROLIMUS USP/EP/BP
  • ZOTAROLIMUS Impurities
  • Zotarolimus, 10 mM in DMSO
  • 221877-54-9
  • C52H79N5O12
  • Inhibitors
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals