| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
In healthy male volunteers, the effects of the phosphodiesterase inhibitor Tibenelast and a placebo were examined in relation to changes in heart rate, cAMP, and norepinephrine levels brought on by isoproterenol. While norepinephrine and cAMP levels remain unchanged with medication, Tillest enhances the heart rate response to isoproterenol infusion [1].
|
|---|---|
| ln Vivo |
Strong oral active substance tibenelast effectively prevents anaphylactic shock brought on by high-dosage antigen aerosols. Bronchoconstriction was seen with a decrease in dynamic compliance (Cdyn) and an increase in lung resistance (RL) after a lesser aerosol challenge of 0.05 mg/mL. Tibasilast 25 mg/kg given orally stopped these alterations. Tibenelast administered intravenously is ten times more effective than aminophylline; when combined with epinephrine, tibenelast at a dose of 1 mg/kg helps restore lung function. Combining tibasilast with epinephrine improves its oral dose-response profile. Treatment for asthma and other respiratory conditions may benefit with tilbest [2].
|
| References |
|
| Molecular Formula |
C13H13O4S-.NA+
|
|---|---|
| Molecular Weight |
288.29472
|
| Exact Mass |
288.043
|
| CAS # |
105102-18-9
|
| PubChem CID |
23700081
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
440.8ºC at 760mmHg
|
| Flash Point |
220.4ºC
|
| Vapour Pressure |
1.52E-08mmHg at 25°C
|
| LogP |
2.062
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
19
|
| Complexity |
302
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ILEWAUWOUIHKID-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C13H14O4S.Na/c1-3-16-9-5-8-6-12(13(14)15)18-11(8)7-10(9)17-4-2;/h5-7H,3-4H2,1-2H3,(H,14,15);/q;+1/p-1
|
| Chemical Name |
sodium;5,6-diethoxy-1-benzothiophene-2-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~173.44 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
