| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
CCR4
CCR4 (CC-chemokine receptor 4). AZD2098 is a potent and specific CCR4 receptor antagonist. It has pIC50 values of 7.8, 8.0, 8.0, and 7.6 for the human CCR4 receptor. By blocking this receptor, the compound inhibits the chemotaxis of CCR4-expressing immune cells, such as Th2 cells and Tregs, which are implicated in allergic and inflammatory responses. |
|---|---|
| ln Vitro |
With pIC50s of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primary human Th2 cells, respectively, AZD2098 potently suppresses chemokine-induced cellular responses[1].
AZD2098 is a potent and selective CCR4 antagonist with pIC50 values of 7.8, 8.0, 8.0, and 7.6. By blocking the CCR4 receptor, it inhibits the migration of CCR4-expressing immune cells. This makes it a valuable compound for studying the role of CCR4 in inflammatory and autoimmune diseases, such as asthma and allergic rhinitis. |
| ln Vivo |
Ovalbumin-sensitized rats treated with AZD2098 (73.5-5.0 μg/kg; po; BID; twice a day; 1 hour before and every 12 hours after antigen challenge) show effective suppression of antigen-induced inflammatory response, with alterations peaking at 7.5 µmol/kg following a dosage of 0.22 µmol/kg.
In vivo, AZD2098 is used to study the role of CCR4 in disease. By blocking this receptor, the compound can modulate immune cell trafficking and reduce inflammation. It has been investigated for the treatment of allergic rhinitis and asthma. Its efficacy would be assessed in animal models of these diseases by measuring inflammatory cell infiltration and disease severity. |
| Enzyme Assay |
In vitro binding assays are used to characterize the interaction of AZD2098 with the CCR4 receptor. Typically, radioligand binding assays are performed using membranes from cells expressing the human CCR4 receptor. The compound's ability to displace a labeled CCR4 ligand is measured to determine its binding affinity, which is reported as pIC50 values.
|
| Cell Assay |
Cellular assays for CCR4 antagonists involve using cells that express CCR4, such as primary T cells or cell lines. These cells are treated with the compound and then stimulated with a CCR4 ligand, such as CCL17 or CCL22. The inhibition of cell migration, or chemotaxis, is then measured to assess the compound's functional antagonism.
|
| Animal Protocol |
Animal/Disease Models: Brown-Norway rats[1]
Doses: 73.5 µg/kg, 250.6 µg/kg, 735.2 µg/kg, 1.0 mg/kg, 2.5 mg/kg, 5.0 mg/kg Route of Administration: Oral administration; twice a day; 1 hour before and every 12 hrs (hours) after antigen challenge Experimental Results: Exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats. In vivo efficacy of AZD2098 is evaluated in animal models of asthma or allergic rhinitis. The compound is administered, and its effects on airway inflammation, hyperresponsiveness, and other disease parameters are assessed. By blocking CCR4, the compound is expected to reduce the recruitment of Th2 cells and other inflammatory cells to the site of inflammation. |
| ADME/Pharmacokinetics |
AZD2098 is a small molecule with the molecular formula C11H9Cl2N3O3S and a molecular weight of 334.18.【12†9】【12†21】【12†25-L26】 Its pharmacokinetic properties, such as oral bioavailability, would be key factors for its utility in in vivo studies. As a research compound, its potency and selectivity for CCR4 are its primary characteristics.
|
| Toxicity/Toxicokinetics |
No specific toxicity data is available for AZD2098. As a CCR4 antagonist, its safety profile would be an important consideration. Potential toxicities could be related to the modulation of immune cell trafficking. Standard preclinical toxicology studies would be needed to evaluate its safety for potential therapeutic applications.
|
| References | |
| Additional Infomation |
AZD2098 (CAS#: 566203-88-1) is a potent and selective antagonist of the CCR4 receptor. It has pIC50 values ranging from 7.6 to 8.0 for the human receptor. It is used as a research tool for studying inflammatory and autoimmune diseases. It is not approved for clinical use.
|
| Molecular Formula |
C11H9CL2N3O3S
|
|---|---|
| Molecular Weight |
334.18
|
| Exact Mass |
332.974
|
| CAS # |
566203-88-1
|
| PubChem CID |
10308720
|
| Appearance |
White to off-white solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
489.3±55.0 °C at 760 mmHg
|
| Flash Point |
249.7±31.5 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.628
|
| LogP |
3.32
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
20
|
| Complexity |
418
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=NC=CN=C1NS(=O)(=O)C2=C(C(=CC=C2)Cl)Cl
|
| InChi Key |
FLSMVCMSUNISFK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H9Cl2N3O3S/c1-19-11-10(14-5-6-15-11)16-20(17,18)8-4-2-3-7(12)9(8)13/h2-6H,1H3,(H,14,16)
|
| Chemical Name |
2,3-dichloro-N-(3-methoxypyrazin-2-yl)benzenesulfonamide
|
| 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 |
| 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: 100 mg/mL (299.24 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.48 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: ≥ 2.5 mg/mL (7.48 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 | 2.9924 mL | 14.9620 mL | 29.9240 mL | |
| 5 mM | 0.5985 mL | 2.9924 mL | 5.9848 mL | |
| 10 mM | 0.2992 mL | 1.4962 mL | 2.9924 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
