Zotarolimus
Based on 4 publication(s) in Google Scholar
Zotarolimus (ABT-578) is a derivative of Rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 221877-54-9
- Formel: C52H79N5O12
- Molecular Weight:966.21
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zotarolimus
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | IC50 |
1400 nM
Compound: 3
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Antiproliferative activity in Lewis rat lymph node cells in rat mixed lymphocyte reaction
Antiproliferative activity in Lewis rat lymph node cells in rat mixed lymphocyte reaction
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[PMID: 16185865] |
| T-cell | IC50 |
2 nM
Compound: 3
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T-cell antiproliferative activity in human mixed lymphocyte reaction
T-cell antiproliferative activity in human mixed lymphocyte reaction
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[PMID: 16185865] |
In Vitro
Zotarolimus (0.01-1000 nM) potently inhibits the binding of an ascomycin derivative to immobilized FKBP12 in a concentration-dependent manner with an IC50 value of 2.57 nM in the FKBP binding affinity assay[1].
Zotarolimus (0.01-1000 nM; 2 days) inhibits Concanavalin A-induced human and rat T cells proliferation in a concentration-dependent manner with IC50 values of 7.0 nM and 1337 nM, respectively[1].
Zotarolimus (v0.01-1000 nM; 2 days) inhibits human coronary artery smooth muscle cell proliferation in a concentration-dependent manner with an IC50 value of 0.8 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (about 130 g) induced delayed-type hypersensitivity (DTH) model[1].
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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))
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Administration:Oral administration, on days 1, 4, 5, 6, and 7
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Result:Inhibited the rat adjuvant-induced DTH response in a dose-dependent manner.
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Animal Model:Male Lewis rats (about 220 g) bearing autoimmune encephalomyelitis (EAE)[1].
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Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
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Administration:Oral administration, once daily, for 13 days
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Result:Inhibited the rat EAE in a dose-dependent manner.
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Animal Model:Lewis rats bearing heterotopic ear-heart transplant[1].
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Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
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Administration:Oral administration, once daily, for 13 days
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Result:Caused a dose-related delay in cardiac allograft rejection.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 221877-54-9
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Appearance Solid
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Molecular Weight 966.21
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Formel C52H79N5O12
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Color White to light yellow
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SMILES
CO[C@H]1[C@@H](N2C=NN=N2)CC[C@@H](C[C@H]([C@@](CC([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H]3C)C)=O)OC)O)\C)C)=O)([H])OC([C@@](CCCC4)([H])N4C(C([C@](O[C@]5([H])C[C@@H](/C(C)=C/C=C/C=C/3)OC)([C@@H](CC5)C)O)=O)=O)=O)C)C1
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Synonyms
ABT-578; A 179578
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Int Immunopharmacol
Zotarolimus alleviates post-trabeculectomy fibrosis via dual functions of anti-inflammation and regulating AMPK/mTOR axis. [Abstract]2024 Sep 19;142(Pt B):113176. PMID: 39303539 -
J Cell Sci
FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. [Abstract]2019 May 20;132(10):jcs227777. PMID: 31028177 -
Acta Trop
Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo. [Abstract]2020 Dec:212:105708. PMID: 32956634
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (103.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (2.59 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sandra E Burke, et al. Zotarolimus (ABT-578) eluting stents. Adv Drug Deliv Rev. 2006 Jun 3;58(3):437-46. [Content Brief]
[2]. Zotarolimus, a novel sirolimus analogue with potent anti-proliferative activity on coronary smooth muscle cells and reduced potential for systemic immunosuppression. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0350 mL | 5.1749 mL | 10.3497 mL | 25.8743 mL |
| 5 mM | 0.2070 mL | 1.0350 mL | 2.0699 mL | 5.1749 mL | |
| 10 mM | 0.1035 mL | 0.5175 mL | 1.0350 mL | 2.5874 mL | |
| 15 mM | 0.0690 mL | 0.3450 mL | 0.6900 mL | 1.7250 mL | |
| 20 mM | 0.0517 mL | 0.2587 mL | 0.5175 mL | 1.2937 mL | |
| 25 mM | 0.0414 mL | 0.2070 mL | 0.4140 mL | 1.0350 mL | |
| 30 mM | 0.0345 mL | 0.1725 mL | 0.3450 mL | 0.8625 mL | |
| 40 mM | 0.0259 mL | 0.1294 mL | 0.2587 mL | 0.6469 mL | |
| 50 mM | 0.0207 mL | 0.1035 mL | 0.2070 mL | 0.5175 mL | |
| 60 mM | 0.0172 mL | 0.0862 mL | 0.1725 mL | 0.4312 mL | |
| 80 mM | 0.0129 mL | 0.0647 mL | 0.1294 mL | 0.3234 mL | |
| 100 mM | 0.0103 mL | 0.0517 mL | 0.1035 mL | 0.2587 mL |
Zotarolimus Related Classifications
HY-12424 Related Classifications
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