ChemicalBook > CAS DataBase List > ZOTAROLIMUS

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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221877-54-9, ZOTAROLIMUSRelated Search:

AZD 3759 (2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol Zonisamide Z-NLE-OH ZM 336372 ZM 39923 HYDROCHLORIDE Z-NVA-OH Z-N-Methyl-D-valine Z-ORN(BOC)-OH ZPCK Tepotinib Saracatinib Dasatinib Trametinib Epothilone B Ruxolitinib ZOSUQUIDAR TRIHYSROCHLORIDE Rapamycin

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