| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
CCR4
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|---|---|
| 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].
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| 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.
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| 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. |
| References |
[1]. Kindon N, et al. Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists. ACS Med Chem Lett. 2017 Sep 1;8(9):981-986.
[2]. Asher Mullard. Cancer charity sees success re-prioritizing industry's shelved compounds. Nat Rev Drug Discov. 2014 May;13(5):319-21. |
| Molecular Formula |
C11H9CL2N3O3S
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|---|---|
| Molecular Weight |
334.18
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| CAS # |
566203-88-1
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| SMILES |
ClC1C(=C([H])C([H])=C([H])C=1S(N([H])C1C(=NC([H])=C([H])N=1)OC([H])([H])[H])(=O)=O)Cl
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (299.24 mM)
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|---|---|
| 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.
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