2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Tibenelast sodium

Tibenelast sodium  (Synonyms: LY 186655)

Cat. No.: HY-101705 Purity: 99.66%
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Tibenelast sodium is a phosphodiesterase inhibitor.

For research use only. We do not sell to patients.

Tibenelast sodium Chemical Structure

Tibenelast sodium Chemical Structure

CAS No. : 105102-18-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Tibenelast sodium:

Tibenelast sodium Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tibenelast sodium is a phosphodiesterase inhibitor.

IC50 & Target

phosphodiesterase[1]
In Vitro

The effect of the phosphodiesterase inhibitor Tibenelast, and placebo on isoproterenol-induced changes in heart rate, cAMP and norepinephrine levels in normal male volunteers is studied. Tibenelast increases the heart rate response to isoproterenol infusion, whereas norepinephrine and cAMP levels are not different in any treatment[1].

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

Tibenelast sodium Related Antibodies
In Vivo

Tibenelast is a potent orally active compound against anaphylactic shock induced by high dose antigen aerosol. When a lower aerosol challenge (0.05 mg/mL) is employed, bronchoconstriction is observed with a concomitant increase in lung resistance (RL) and a fall in dynamic compliance (Cdyn). Tibenelast at 25 mg/kg p.o. prevents these changes. Tibenelast is 10 times more potent than Aminophylline by i.v. administration; normalization of pulmonary function is achieved at 1 mg/kg i.v. Tibenelast is synergistic with epinephrine. The oral dose response curve of Tibenelast is enhanced with the co-administration of epinephrine. Tibenelast may be of significant value in the treatment of asthma and other respiratory diseases[2].

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

288.29

Formula

C13H13NaO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=CC(OCC)=C(OCC)C=C2S1)[O-].[Na+]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (173.44 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 3.4687 mL 17.3436 mL 34.6873 mL
5 mM 0.6937 mL 3.4687 mL 6.9375 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 (sealed storage, away from moisture). 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.67 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: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 3.4687 mL 17.3436 mL 34.6873 mL 86.7182 mL
5 mM 0.6937 mL 3.4687 mL 6.9375 mL 17.3436 mL
10 mM 0.3469 mL 1.7344 mL 3.4687 mL 8.6718 mL
15 mM 0.2312 mL 1.1562 mL 2.3125 mL 5.7812 mL
20 mM 0.1734 mL 0.8672 mL 1.7344 mL 4.3359 mL
25 mM 0.1387 mL 0.6937 mL 1.3875 mL 3.4687 mL
30 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8906 mL
40 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1680 mL
50 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.7344 mL
60 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
80 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
100 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
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Tibenelast sodium 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:

Tibenelast105102-18-9LY 186655LY186655LY-186655Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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