2. Anti-infection Apoptosis Neuronal Signaling Membrane Transporter/Ion Channel
  3. Bacterial Antibiotic Apoptosis Calcium Channel
  4. Tilmicosin

Tilmicosin  (Synonyms: LY-177370; EL-870)

製品番号: HY-B0905 純度: 98.0%
COA 取扱説明書 Technical Support

Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects.

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Tilmicosin

Tilmicosin 構造式

CAS 番号 : 108050-54-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 33 在庫あり
Solution
10 mM * 1 mL in DMSO USD 33 在庫あり
Solid
100 mg $30 在庫あり
500 mg $60 在庫あり
1 g   お問い合わせ  
5 g   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 5 publication(s) in Google Scholar

Other Forms of Tilmicosin:

Tilmicosin 関連抗体

Top Publications Citing Use of Products

Antibiotic アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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製品説明

Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects[1][2][3][4][5][6].

IC50 & Target[3]

COX-2

 

体外実験

Tilmicosin (0-7 μg/mL; 16-18 h) has the MIC for 90% of Staphylococcus aureus isolates from the bovine udder of 0.78 μg/mL[1].
Tilmicosin (0.5μg /mL; 2 h) induces apoptosis of bovine neutrophils[2].
Tilmicosin (5-20 μg/mL; 18 h) inhibits the expression of COX-2 and iNOS in LPS (HY-D1056) treated macrophages, and affects the secretion of cytokines[3].

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

Tilmicosin 関連抗体

RT-PCR[3]

Cell Line: LPS (HY-D1056) treated RAW264.7 cells
Concentration: 5, 10 and 20 μg/mL
Incubation Time: 18 h
Result: Reduced the levels of COX-2 and iNOS.
体内実験

Tilmicosin (75 mg/kg; subcutaneous injection; single dose) induces cardiotoxicity in mice[4].
Pharmacokinetic Analysis in lung tissues of the M. gallisepticum infected chickens[5]

Route Dose (mg/kg) t1/2kel (h) Tmax (h) Cmax (μg/g) AUC (μg·h/g) MRT (h) CL/F (1/h/kg)
p.o. 1 48.46 12.00 0.12 13.62 53.60 0.09
p.o. 30 50.60 12.00 6.19 464.23 50.88 0.06

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

Animal Model: Male albino mice[4]
Dosage: 75 mg/kg
Administration: Subcutaneous injection (s.c.); single dose
Result: Significantly increased cardiac injury markers in serum (LDH, CK and CK-MB).
Significantly increased the cardiac MDA content and decreased cardiac GSH, SOD, CAT and TAC.
分子量

869.13

分子式

C46H80N2O13
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]([C@@H](CC1=O)O)[C@H]([C@H](C[C@H](C(/C=C/C(C)=C/[C@H](CO[C@H](O[C@H](C)[C@@H](O)[C@H]2OC)[C@@H]2OC)[C@@H](CC)O1)=O)C)CCN(C[C@H](C)C3)C[C@H]3C)O[C@@](O[C@H](C)[C@@H](O)[C@@H]4N(C)C)([H])[C@@H]4O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

1M HCl : 100 mg/mL (115.06 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 100 mg/mL (115.06 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 1.1506 mL 5.7529 mL 11.5058 mL
5 mM 0.2301 mL 1.1506 mL 2.3012 mL
10 mM 0.1151 mL 0.5753 mL 1.1506 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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 (2.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (2.88 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
1M HCl / DMSO 1 mM 1.1506 mL 5.7529 mL 11.5058 mL 28.7644 mL
5 mM 0.2301 mL 1.1506 mL 2.3012 mL 5.7529 mL
10 mM 0.1151 mL 0.5753 mL 1.1506 mL 2.8764 mL
15 mM 0.0767 mL 0.3835 mL 0.7671 mL 1.9176 mL
20 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
25 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1506 mL
30 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
40 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
50 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
60 mM 0.0192 mL 0.0959 mL 0.1918 mL 0.4794 mL
80 mM 0.0144 mL 0.0719 mL 0.1438 mL 0.3596 mL
100 mM 0.0115 mL 0.0575 mL 0.1151 mL 0.2876 mL
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Tilmicosin 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:

Tilmicosin108050-54-0LY-177370 EL-870LY177370LY 177370EL870EL 870EL-870BacterialAntibioticApoptosisCalcium ChannelCa2+ channelsCa channelsneutrophilsmacrophagesInhibitorinhibitorinhibit

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