| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Tipelukast is the leukotriene receptor, specifically the sulfidopeptide leukotriene receptor. By antagonizing this receptor, tipelukast blocks the action of leukotrienes, which are inflammatory mediators involved in asthma, allergic rhinitis, and other inflammatory conditions. This reduces bronchoconstriction and inflammation in the airways.
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|---|---|
| ln Vitro |
Tipelukast prevents the guinea pig lung cell membrane's [3H] LTD4 receptor from binding to it (IC50 = 2.3 μmol) [2].
In vitro, Tipelukast has been shown to be a sulfidopeptide leukotriene receptor antagonist. It inhibits the action of leukotrienes, reducing inflammatory responses in various cell types. The compound's activity has been confirmed in various in vitro models. |
| ln Vivo |
Five minutes and fifteen minutes after the aerosolized antigen challenge, guinea pigs were given UNDW via inhalation. Tipelukast markedly altered the bronchoconstriction induced by UNDW [1]. In guinea pigs, tepelukast (1 and 5 mg/kg) administered intravenously 15 minutes post-antigen challenge reduces propranolol-induced bronchoconstriction (PIB) in a dose-dependent manner [2].
In vivo, Tipelukast (10, 30, and 50 mg/kg) reduces the frequency of bladder voids, increases the intercontractile interval, and decreases the number of non-voiding contractions in a rat model of bladder hyperactivity induced by ovalbumin-induced mast cell stimulation. It is used for the treatment of asthma and allergic rhinitis. |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for Tipelukast involve studying its binding affinity for the leukotriene receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the leukotriene receptor. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the affinity.
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| Cell Assay |
In vitro cell-based assays for Tipelukast are performed using various cell types, such as mast cells and airway smooth muscle cells. Cells are treated with the compound, and the production of inflammatory mediators is measured. The compound's effects on leukotriene-induced responses, such as calcium mobilization and cell contraction, are assessed.
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| Animal Protocol |
In vivo animal experiments for Tipelukast are conducted using rat models of bladder hyperactivity induced by ovalbumin-induced mast cell stimulation. The compound is administered orally, and the frequency of bladder voids, intercontractile interval, and number of non-voiding contractions are measured. These studies confirm the compound's efficacy as an anti-inflammatory agent.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of Tipelukast indicate that it is orally bioavailable. The compound has a molecular weight of 530.67 and a molecular formula of C29H38O7S. The CAS number is 125961-82-2. The IUPAC name is 4-(6-acetyl-3-(3-((4-acetyl-3-hydroxy-2-propylphenyl)thio)propoxy)-2-propylphenoxy)butanoic acid. Powder is stable when stored at -20°C for 3 years.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for Tipelukast are limited. As a leukotriene receptor antagonist, it is generally well-tolerated at therapeutic doses. Common side effects may include headache and gastrointestinal disturbances. The compound is for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
Tipelukast is an aromatic ketone. Tipelukast is being investigated for the treatment of idiopathic pulmonary fibrosis (IPF).
Other information: Tipelukast is also known as KCA 757 and MN-001. It is a sulfidopeptide leukotriene receptor antagonist and an orally bioavailable anti-inflammatory agent. The compound is used for the treatment of asthma. Its CAS number is 125961-82-2. |
| Molecular Formula |
C29H38O7S
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|---|---|
| Molecular Weight |
530.67
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| Exact Mass |
530.233
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| CAS # |
125961-82-2
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| PubChem CID |
9893228
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
735.3±60.0 °C at 760 mmHg
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| Flash Point |
398.5±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.582
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| LogP |
7.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
37
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KPWYNAGOBXLMSE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H38O7S/c1-5-9-23-25(14-12-22(20(4)31)29(23)36-16-7-11-27(32)33)35-17-8-18-37-26-15-13-21(19(3)30)28(34)24(26)10-6-2/h12-15,34H,5-11,16-18H2,1-4H3,(H,32,33)
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| Chemical Name |
4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenyl)sulfanylpropoxy]-2-propylphenoxy]butanoic acid
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| Synonyms |
KCA757; MN-001; KCA-757
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol : ~1 mg/mL (~1.88 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8844 mL | 9.4221 mL | 18.8441 mL | |
| 5 mM | 0.3769 mL | 1.8844 mL | 3.7688 mL | |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8844 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.
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