| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
The targets of Andolast include phosphodiesterase (PDE) and potassium channels. Andolast inhibits cAMP-phosphodiesterase with an IC₅₀ of 50 μM. By inhibiting PDE, Andolast prevents the breakdown of cyclic AMP (cAMP), leading to increased intracellular cAMP levels. Elevated cAMP activates protein kinase A (PKA), which in turn mediates smooth muscle relaxation and anti-inflammatory effects. Andolast has also been identified as a potassium channel opener, specifically a calcium-activated potassium channel opener. Potassium channel opening contributes to smooth muscle relaxation and bronchodilation. The compound's dual mechanism of action makes it effective in treating asthma and allergic conditions.
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| ln Vitro |
In vitro, Andolast inhibits cAMP-phosphodiesterase with an IC₅₀ of 50 μM. This inhibition leads to increased cAMP levels in target cells, which promotes smooth muscle relaxation and reduces inflammatory responses. The compound's anti-allergic effects can be evaluated in vitro by measuring its ability to inhibit histamine release from mast cells or to suppress cytokine production in activated immune cells. Andolast's potassium channel opening activity can be assessed using patch-clamp electrophysiology or fluorescence-based membrane potential assays. The compound demonstrates anti-allergic activity in various in vitro models of allergic inflammation.
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| ln Vivo |
Andolast (CR 2039) (intravenous or intramuscular injection) reduces passive cutaneous anaphylaxis (PCA) in rats with an ED50 of 0.1 mg/kg[1]. CR 2039 (10-100 mg/kg; intravenously or intramuscularly) reduces alterations in microvascular permeability in a sensitized guinea pig model of allergic conjunctivitis [1]. CR 2039 (0-1000 μM; intravenous injection) dose-dependently inhibits guinea pig lung cAMP-phosphodiesterase with an IC50 value of 50 μM [1].
In vivo, Andolast has demonstrated efficacy in animal models of asthma and allergic inflammation. The compound is administered orally and has been shown to improve airflow and control asthma symptoms. In clinical studies, Andolast proved significantly more effective than placebo in improving airflow and in controlling asthma symptoms both during day and night. The compound has been investigated up to Phase 3 clinical trials for the treatment of rhinitis. These studies support the compound's potential as an anti-allergic therapeutic. Further in vivo studies are needed to fully characterize its efficacy in various allergic conditions. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for Andolast focus on its phosphodiesterase inhibitory activity. PDE enzyme activity can be measured using colorimetric or radiometric assays that detect the hydrolysis of cAMP or cGMP. Andolast's IC₅₀ of 50 μM for cAMP-PDE inhibition is determined from dose-response curves. Selectivity profiling against different PDE isoforms (PDE1-PDE11) can be performed to determine the compound's specificity. Potassium channel opening activity can be assessed using electrophysiological techniques such as patch-clamp or two-electrode voltage clamp in cells expressing potassium channels. These methods are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Andolast evaluate its anti-allergic and anti-inflammatory effects. Mast cells or basophils are treated with Andolast at various concentrations and stimulated with allergens or calcium ionophores. Histamine release is measured by ELISA or fluorometric assays. Cytokine production (e.g., IL-4, IL-5, IL-13, TNF-α) can be measured in activated immune cells using ELISA or multiplex assays. Smooth muscle cell relaxation can be assessed by measuring intracellular calcium levels or cell contraction assays. Cell viability assays (MTT or CCK-8) are performed to evaluate cytotoxicity. Standard cell culture conditions are used with appropriate media and supplementation.
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| Animal Protocol |
Animal/Disease Models: Male Hartley guinea pig (300-500 g) [1]
Doses: 10-100 mg/kg Route of Administration: intramuscularinjection; IV Experimental Results: Demonstrated dependence on lgE induced by aerosolized antigen in anesthetized guinea pigs Dose-related significant protective effect against bronchial allergic reactions. Dose-dependently delays the onset of aerosolized antigen-induced bronchoconstriction. In vivo animal studies for Andolast utilize models of allergic airway inflammation. Mice or rats are sensitized and challenged with allergens (e.g., ovalbumin) to induce airway hyperresponsiveness and inflammation. Andolast is administered orally at various doses (typically 1-100 mg/kg). Airway resistance is measured using plethysmography, and bronchoalveolar lavage fluid is analyzed for inflammatory cell infiltration and cytokine levels. Lung histology is performed to assess tissue inflammation and remodeling. Clinical studies in humans have demonstrated efficacy in asthma and rhinitis. All procedures must comply with institutional animal care guidelines. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Andolast have been characterized in preclinical and clinical studies. The compound is orally bioavailable and has been evaluated in clinical trials. The molecular weight is 333.31 g/mol. The compound's half-life, Cmax, AUC, and clearance are available from published studies. Andolast has been investigated up to Phase 3 clinical trials for rhinitis, indicating favorable pharmacokinetic properties. The compound is for research use only and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
The toxicity profile of Andolast has been evaluated in preclinical and clinical studies. The compound has been investigated up to Phase 3 clinical trials, indicating an acceptable safety profile. Common adverse effects may include mild gastrointestinal disturbances or headache. The compound is for research use only and is not approved for clinical use. Standard safety precautions for handling pharmaceutical compounds apply, including the use of personal protective equipment and working in a chemical fume hood.
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| References |
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| Additional Infomation |
Additional information: Andolast is also known as CR-2039 and Dizolast. It has the molecular formula C₁₅H₁₁N₉O and molecular weight 333.31. The compound is a small molecule drug developed by Rottapharm Madaus. Andolast functions as a cAMP-phosphodiesterase inhibitor (IC₅₀ = 50 μM) and a potassium channel opener. The compound has been investigated for the treatment of bronchial asthma, COPD, and rhinitis. Andolast proved significantly more effective than placebo in improving airflow and controlling asthma symptoms. The compound has been evaluated up to Phase 3 clinical trials for rhinitis. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C15H11N9O
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| Molecular Weight |
333.30754
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| Exact Mass |
333.109
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| CAS # |
132640-22-3
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| Related CAS # |
Andolast;143330-46-5
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| PubChem CID |
65970
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| Appearance |
White to off-white solid powder
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| Density |
1.551g/cm3
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| Index of Refraction |
1.748
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| LogP |
1.683
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
448
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VXEBMQZDPONDFB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11N9O/c25-15(11-3-1-9(2-4-11)13-17-21-22-18-13)16-12-7-5-10(6-8-12)14-19-23-24-20-14/h1-8H,(H,16,25)(H,17,18,21,22)(H,19,20,23,24)
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| Chemical Name |
4-(2H-tetrazol-5-yl)-N-[4-(2H-tetrazol-5-yl)phenyl]benzamide
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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) |
DMSO : ~50 mg/mL (~150.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0002 mL | 15.0011 mL | 30.0021 mL | |
| 5 mM | 0.6000 mL | 3.0002 mL | 6.0004 mL | |
| 10 mM | 0.3000 mL | 1.5001 mL | 3.0002 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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