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

Tibenelast sodium (Synonyms: LY 186655)

Cat. No.: HY-101705 Purity: 99.64%
Handling Instructions

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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5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
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25 mg USD 600 In-stock
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50 mg USD 1050 In-stock
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100 mg USD 1750 In-stock
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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].

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

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].

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

Molecular Weight

288.29

Formula

C₁₃H₁₃NaO₄S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (173.44 mM; Need ultrasonic)

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
10 mM 0.3469 mL 1.7344 mL 3.4687 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
Tibenelast sodium
Cat. No.:
HY-101705
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