| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
CGP 35949 targets the leukotriene receptor, specifically acting as an LTD₄ antagonist. Leukotriene D₄ is a potent bronchoconstrictor and pro-inflammatory mediator involved in asthma pathogenesis. By blocking LTD₄ receptors, CGP 35949 inhibits leukotriene-mediated bronchoconstriction and inflammation. The compound also has phospholipase inhibitory activity, which may contribute to its anti-inflammatory effects by reducing the production of inflammatory mediators.
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| ln Vitro |
In vitro, CGP 35949 demonstrates LTD₄ antagonist activity and phospholipase inhibitory activity. The compound's ability to block LTD₄ receptors has been characterized in receptor binding and functional assays. Specific IC₅₀ values for LTD₄ antagonism and phospholipase inhibition are documented in the literature. The compound is soluble in DMSO at 5.11 mg/mL (10 mM). It has a purity of >99%.
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| ln Vivo |
In vivo, CGP 35949 has been investigated for the treatment of asthma. As an LTD₄ antagonist with phospholipase inhibitory activity, it has the potential to reduce both bronchoconstriction and airway inflammation in asthmatic patients. The compound's efficacy in asthma models has been demonstrated in preclinical studies. Further clinical development would be required to establish its full therapeutic potential in humans.
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| Enzyme Assay |
Leukotriene receptor binding assays are performed using membrane preparations from cells or tissues expressing LTD₄ receptors. Radioligand displacement assays use [³H]-LTD₄ or other appropriate radiolabeled ligands. CGP 35949 is tested at various concentrations, and IC₅₀/Ki values are calculated. Phospholipase inhibition assays use purified enzyme preparations and appropriate substrates. Enzyme activity is measured by detecting reaction products using chromatographic or spectrophotometric methods.
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| Cell Assay |
In vitro cellular assays use cell lines expressing leukotriene receptors or inflammatory cells such as mast cells, eosinophils, or macrophages. Cells are stimulated with inflammatory stimuli and treated with CGP 35949 at various concentrations. Leukotriene production and inflammatory mediator release are measured by ELISA. Cell viability is assessed by MTT assay. The compound is dissolved in DMSO for stock solutions and diluted in culture media.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of asthma, including ovalbumin-induced airway hyperresponsiveness and allergic airway inflammation models. CGP 35949 is administered orally, intraperitoneally, or by inhalation. Endpoints include airway resistance, bronchoalveolar lavage inflammatory cell counts, cytokine levels, and histopathological assessment of lung tissues. Pharmacokinetic studies may be conducted to support efficacy evaluations.
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| ADME/Pharmacokinetics |
CGP 35949 has a molecular weight of 509.92 and molecular formula C₂₃H₂₅ClN₅NaO₅ with CAS number 111130-13-3. It is soluble in DMSO at 5.11 mg/mL (10 mM). The compound has a purity of >99%. For storage, it should be kept at -20°C, and if dissolved in non-DMSO solvents, aliquots should be stored at -80°C for up to 6 months. Specific pharmacokinetic parameters are documented in the literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for CGP 35949 are not extensively documented in the available literature. As a research compound for asthma treatment, its safety profile is still being characterized. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only and not for human therapeutic applications. The compound should be handled in a well-ventilated area with appropriate personal protective equipment.
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| References | |
| Additional Infomation |
CGP 35949 is an LTD₄ antagonist with phospholipase inhibitory activity developed as a potential treatment for asthma. By blocking LTD₄ receptors and inhibiting phospholipase, it targets both bronchoconstriction and airway inflammation, representing a dual mechanism approach to asthma therapy. The compound has been studied in preclinical models and represents a new approach to the treatment of asthma. It is commercially available for research purposes only.
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| Molecular Formula |
C23H25CLN5NAO5
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|---|---|
| Molecular Weight |
509.92
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| Exact Mass |
509.144
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| CAS # |
111130-13-3
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| PubChem CID |
23693560
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
597.3ºC at 760 mmHg
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| Flash Point |
315ºC
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| Vapour Pressure |
4.11E-15mmHg at 25°C
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| LogP |
4.724
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].CCCC1=C(OCCCOC2C=C(NC(C3=NN=N[N-]3)=O)C(C)=CC=2Cl)C=CC(C(=O)C)=C1O
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| InChi Key |
CJDFUZGGLMRUHB-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C23H26ClN5O5.Na/c1-4-6-16-19(8-7-15(14(3)30)21(16)31)33-9-5-10-34-20-12-18(13(2)11-17(20)24)25-23(32)22-26-28-29-27-22;/h7-8,11-12H,4-6,9-10H2,1-3H3,(H3,25,26,27,28,29,30,31,32);/q;+1/p-1
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| Chemical Name |
sodium;N-[5-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]-4-chloro-2-methylphenyl]-1,2,3-triaza-4-azanidacyclopenta-2,5-diene-5-carboxamide
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| Synonyms |
Cgp35949 Cgp-35949 Cgp 35949
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.9611 mL | 9.8055 mL | 19.6109 mL | |
| 5 mM | 0.3922 mL | 1.9611 mL | 3.9222 mL | |
| 10 mM | 0.1961 mL | 0.9805 mL | 1.9611 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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