| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Leukotriene receptor
Verlukast targets the cysteinyl leukotriene receptor 1 (CysLT1 receptor), also known as the leukotriene D4 (LTD4) receptor. By binding to this receptor, it antagonizes the effects of leukotrienes, which are lipid mediators that cause bronchoconstriction, mucus secretion, and inflammation in the airways. |
|---|---|
| ln Vitro |
The leukotriene antagonist MK-0679 caused bronchodilation which lasted for at least nine hours. The average peak improvement in FEV1 was 18% above the predrug baseline, but the bronchodilator response varied between 34% and 5% and was found to correlate strongly with the severity of asthma and aspirin sensitivity [1].
In vitro, Verlukast is a potent LTD4 receptor antagonist. It shows [³H]leukotriene D4 binding in guinea pig lung membranes with an IC50 of 3.2 nM. The pharmacological profile for Verlukast is similar to that of the racemic compound, MK-571. |
| ln Vivo |
The cysteinyl leukotrienes (LTC4, LTD4, and LTE4) have been shown to mediate airway obstruction evoked by several factors which trigger asthmatic reactions--for example, allergen and exercise. Accordingly, drugs which block the action or formation of these leukotrienes are being evaluated as a new treatment of asthma. Elevated production of leukotrienes has been reported in asthmatic subjects who are intolerant to aspirin and related nonsteroidal anti-inflammatory drugs. In this study the influence of the specific leukotriene receptor antagonist MK-0679 was tested on basal airway function in asthmatic patients with documented aspirin intolerance [1].
In vivo, Verlukast has the potential for the treatment of asthma. It causes bronchodilation that lasts for at least nine hours. In patients, FEV1 improves by 18% from baseline. It was in clinical development for the treatment of asthma. |
| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Verlukast are performed using membrane preparations from guinea pig lung or cells expressing the human CysLT1 receptor. These membranes are incubated with [³H]leukotriene D4 and varying concentrations of Verlukast. Binding affinity (IC50 or Ki) is determined by competitive displacement of the radiolabeled ligand.
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| Cell Assay |
In vitro cell-based experiments for Verlukast are conducted using cells expressing the human CysLT1 receptor (e.g., HEK-293 cells). Cells are seeded in plates and loaded with a calcium-sensitive dye. They are then treated with Verlukast at various concentrations, followed by stimulation with leukotriene D4. Calcium mobilization is measured to assess receptor antagonism, and IC50 values are calculated from inhibition curves.
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| Animal Protocol |
In vivo animal experiments for Verlukast are performed in animal models of asthma (e.g., ovalbumin-sensitized guinea pigs). Verlukast is administered orally. Airway hyperresponsiveness, bronchoconstriction, and inflammatory markers are assessed. Bronchodilation and the duration of action are evaluated.
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| ADME/Pharmacokinetics |
Verlukast is orally bioavailable with good systemic exposure. Detailed pharmacokinetic parameters are available from preclinical and clinical studies. It has a half-life suitable for once or twice daily dosing.
|
| Toxicity/Toxicokinetics |
Verlukast is well-tolerated at therapeutic doses in preclinical and clinical studies. No significant toxicity has been reported. It is selective for leukotriene receptors.
|
| References | |
| Additional Infomation |
Verlukast is also known as MK-679 and MK-0679. It is a research compound for asthma. It is the (R)-enantiomer of MK-571 and a potent CysLT1 receptor antagonist. It is not approved for clinical use.
|
| Molecular Formula |
C26H27CLN2O3S2
|
|---|---|
| Molecular Weight |
515.083
|
| Exact Mass |
514.115
|
| Elemental Analysis |
C, 60.63; H, 5.28; Cl, 6.88; N, 5.44; O, 9.32; S, 12.45
|
| CAS # |
120443-16-5
|
| Related CAS # |
Verlukast-d6;153698-86-3
|
| PubChem CID |
6509849
|
| Appearance |
Light yellow to yellow solid
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
712.3±60.0 °C at 760 mmHg
|
| Flash Point |
384.6±32.9 °C
|
| Vapour Pressure |
0.0±2.4 mmHg at 25°C
|
| Index of Refraction |
1.687
|
| LogP |
5.93
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
34
|
| Complexity |
693
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CN(C)C(=O)CCS[C@@H](C1=CC=CC(=C1)/C=C/C2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O
|
| InChi Key |
AXUZQJFHDNNPFG-UXBLZVDNSA-N
|
| InChi Code |
InChI=1S/C26H27ClN2O3S2/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32)/b10-6+
|
| Chemical Name |
Propanoic acid, 3-(((3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)((3-(dimethylamino)-3-oxopropyl)thio)methyl)thio)-, (E)-
|
| Synonyms |
L-668,019; L 668019; L 668,019
|
| 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: > 10 mM
|
|---|---|
| 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 | 1.9414 mL | 9.7072 mL | 19.4145 mL | |
| 5 mM | 0.3883 mL | 1.9414 mL | 3.8829 mL | |
| 10 mM | 0.1941 mL | 0.9707 mL | 1.9414 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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