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  4. Zotarolimus

ゾタロリムス  (Synonyms: Zotarolimus; ABT-578; A 179578)

製品番号: HY-12424 純度: ≥98.0%
COA 取扱説明書 Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Zotarolimus 構造式

ゾタロリムス 構造式

CAS 番号 : 221877-54-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 173 在庫あり
Solution
10 mM * 1 mL in DMSO USD 173 在庫あり
Solid
5 mg USD 94 在庫あり
10 mg USD 163 在庫あり
25 mg USD 343 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 4 publication(s) in Google Scholar

Other Forms of Zotarolimus:

ゾタロリムス 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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[1][2].

体外実験

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.

ゾタロリムス 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
臨床実験
分子量

966.21

分子式

C52H79N5O12
CAS 番号
Appearance

Solid

Color

White to light yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0350 mL 5.1749 mL 10.3497 mL
5 mM 0.2070 mL 1.0350 mL 2.0699 mL
10 mM 0.1035 mL 0.5175 mL 1.0350 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: ≥98.0%

COA (261 KB) HNMR (154 KB)

取扱説明書 (2659 KB)
参考文献

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
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Zotarolimus Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zotarolimus221877-54-9ABT-578 A 179578ABT578ABT 578A179578A 179578A-179578Drug DerivativeDrug derivativeRapamycincoronaryarteryrestenosisdiseaseimmunosuppressantdrug-elutingstentsInhibitorinhibitorinhibit

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製品名:
Zotarolimus
製品番号:
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