2. Metabolic Enzyme/Protease GPCR/G Protein NF-κB Immunology/Inflammation
  3. Lipoxygenase Leukotriene Receptor Reactive Oxygen Species (ROS) MMP
  4. Tremulacin

Tremulacin is a 5-LOX inhibitor. Tremulacin reduces the biosynthesis of LTB4 and slow-reacting substances of anaphylaxis. Tremulacin alleviates carrageenan-induced paw edema in rats, croton oil-induced ear edema in mice, and acetic acid-induced writhing response in mice. Tremulacin inhibits TNF-α-stimulated ROS production and MMP-1 expression, and promotes collagen secretion in human dermal fibroblasts. Tremulacin is investigated for studies on inflammation-related diseases.

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Tremulacin

Tremulacin Chemical Structure

CAS No. : 29836-40-6

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Tremulacin Related Antibodies

Top Publications Citing Use of Products

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5-LOX 12-LOX 15-LOX

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tremulacin is a 5-LOX inhibitor. Tremulacin reduces the biosynthesis of LTB4 and slow-reacting substances of anaphylaxis. Tremulacin alleviates carrageenan-induced paw edema in rats, croton oil-induced ear edema in mice, and acetic acid-induced writhing response in mice. Tremulacin inhibits TNF-α-stimulated ROS production and MMP-1 expression, and promotes collagen secretion in human dermal fibroblasts. Tremulacin is investigated for studies on inflammation-related diseases[1][2][3].

IC50 & Target[1][2]

5-LOX

 

LTB4

 

MMP-1

 

In Vitro

Tremulacin (10 μM; 30 min) inhibits LTB4 biosynthesis by 30% in leukocytes from rat pleural cavities, but exerts no effect on HHT biosynthesis in platelets, and reduces SRS-A biosynthesis by 41% in isolated longitudinal muscle strips from the ileum of sensitized guinea pigs[1].
Tremulacin (1-100 μM; 24 h) reduces cell viability at the concentration of 100 μM[2].
Tremulacin (1-30 μM; pre-incubated for 1 h prior to TNF-α treatment) inhibits TNF-α-induced ROS production in normal human skin fibroblasts, suppresses TNF-α-induced MMP-1 secretion in normal human dermal fibroblasts, and partially restores COLIA1 secretion[2].
Tremulacin exhibits weak antiviral activity against HSV-1 (EC50 = 87 μM), HSV-2 (EC50 = 86 μM) and HIV-1 (EC50 = 52 μM)[3].

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

Tremulacin Related Antibodies

Cell Viability Assay[2]

Cell Line: normal human dermal fibroblasts (HDFs)
Concentration: 1, 3, 10, 30, 100 μM
Incubation Time: 24 h
Result: Showed no significant changes in cell viability at concentrations of 1, 3, 10, and 30 μM.
Caused a significant decrease in cell viability at 100 μM.

ELISA Assay[2]

Cell Line: TNF-α-stimulated normal human dermal fibroblasts (HDFs)
Concentration: 1, 3, 10, 30 μM
Incubation Time: 1 h (pre-incubation before 24 h TNF-α treatment)
Result: Reduced TNF-α-induced MMP-1 secretion to 1.03 ng/mL at 1 μM.
Reduced TNF-α-induced MMP-1 secretion to 1.66 ng/mL at 3 μM.
Reduced TNF-α-induced MMP-1 secretion to 1.28 ng/mL at 10 μM.
Reduced TNF-α-induced MMP-1 secretion to 1.21 ng/mL at 30 μM.
Increased TNF-α-reduced COLIA1 secretion to 0.82 ng/mL at 3 μM.
In Vivo

Tremulacin (100 mg/kg; subcutaneous injection; single dose) inhibits carrageenan-induced paw edema in Wistar rats and suppresses peritoneal leukocyte migration in Wistar rats by 50%[1].
Tremulacin (100 mg/kg; subcutaneous injection; single administration) inhibits croton oil-induced ear swelling in Kunming mice by 43%[1].
Tremulacin (100 mg/kg; subcutaneous injection; single administration) prolongs the latency and reduces the frequency of acetic acid-induced writhing responses in Kunming mice[1].

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

Animal Model: Wistar (male, 180-220 g, carrageenan-induced paw edema model/ sodium carboxymethylcellulose-induced peritoneal leukocyte migration model)[1]
Dosage: 100 mg/kg
Administration: s.c.; single dose
Result: Significantly reduced paw swelling for at least 6 hours, with a maximum inhibition rate of approximately 55%.
Reduced peritoneal leukocyte counts from 1.2×104 cells/mL in controls to 6×103 cells/mL in treated rats, resulting in a 50% inhibition rate.
Animal Model: Kun Ming (male, 18-22 g, croton oil-induced ear edema model)[1]
Dosage: 100 mg/kg
Administration: s.c.; single dose
Result: Decreased ear edema by 43%, reducing the mean ear weight increase from 18.1 mg in controls to 10.3 mg in treated mice.
Animal Model: Kun Ming (male, 18-22 g, acetic acid-induced writhing model)[1]
Dosage: 100 mg/kg
Administration: s.c.; single dose
Result: Increased the mean time to onset of writhing from 2.43 minutes in controls to 3.75 min.
Reduced the mean number of writhing responses over 15 minutes from 34.86 in controls to 19.75.
Molecular Weight

528.50

Formula

C27H28O11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC=C1)O[C@H]([C@H]([C@@H]([C@H](O2)CO)O)O)[C@@H]2OC3=C(C=CC=C3)COC([C@]4(C(CCC=C4)=O)O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.21 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 1.8921 mL 9.4607 mL 18.9215 mL
5 mM 0.3784 mL 1.8921 mL 3.7843 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.73 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 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.73 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:

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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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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.
Purity & Documentation
References

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
DMSO 1 mM 1.8921 mL 9.4607 mL 18.9215 mL 47.3037 mL
5 mM 0.3784 mL 1.8921 mL 3.7843 mL 9.4607 mL
10 mM 0.1892 mL 0.9461 mL 1.8921 mL 4.7304 mL
15 mM 0.1261 mL 0.6307 mL 1.2614 mL 3.1536 mL
20 mM 0.0946 mL 0.4730 mL 0.9461 mL 2.3652 mL
25 mM 0.0757 mL 0.3784 mL 0.7569 mL 1.8921 mL
30 mM 0.0631 mL 0.3154 mL 0.6307 mL 1.5768 mL
40 mM 0.0473 mL 0.2365 mL 0.4730 mL 1.1826 mL
50 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9461 mL
60 mM 0.0315 mL 0.1577 mL 0.3154 mL 0.7884 mL
80 mM 0.0237 mL 0.1183 mL 0.2365 mL 0.5913 mL
100 mM 0.0189 mL 0.0946 mL 0.1892 mL 0.4730 mL
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Tremulacin Related Classifications

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:

Tremulacin29836-40-6LipoxygenaseLeukotriene ReceptorReactive Oxygen Species (ROS)MMPLOXMatrix metalloproteinasescyclooxygenasecarrageenan-induced paw edemacroton oil-induced ear edema5-lipoxygenaseHIV-1acetic acid-induced writhing responsesSlow Reaction Substance of Anaphylaxishuman dermal fibroblastsleukotriene B4HSV-1Inhibitorinhibitorinhibit

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