| 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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| 50mg |
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| Targets |
CCR3 antagonist 1 targets the CCR3 (C-C chemokine receptor type 3) receptor. It is a potent antagonist with an IC50 of 1.8 nM, showing high affinity for this target. The CCR3 receptor is involved in the immune response, particularly in inflammation and allergic reactions, by mediating the chemotaxis of eosinophils and other immune cells.
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| ln Vitro |
In vitro, CCR3 antagonist 1 is characterized by its potent antagonist activity. Its IC50 of 1.8 nM demonstrates high efficacy in blocking the receptor. This is typically assessed in cell-based functional assays by measuring its ability to inhibit CCR3-mediated signaling pathways, such as calcium mobilization or chemotaxis, induced by its natural ligands like eotaxin.
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| ln Vivo |
In vivo, CCR3 antagonist 1 is used in preclinical research models. By blocking the CCR3 receptor, it can reduce the recruitment of eosinophils and other inflammatory cells to sites of inflammation. This makes it a promising candidate for the treatment of allergic diseases like asthma, allergic rhinitis, and atopic dermatitis, as well as other inflammatory conditions.
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| Enzyme Assay |
The in vitro receptor binding assay for CCR3 antagonist 1 is a competitive binding assay. Membranes from cells expressing the human CCR3 receptor are incubated with a radiolabeled ligand, such as [125I]-eotaxin, in the presence of varying concentrations of the antagonist. The amount of radioligand displaced is measured to determine the binding affinity (Ki).
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| Cell Assay |
In vitro cell-based functional assays for CCR3 antagonist 1 involve cells that express the CCR3 receptor, such as human eosinophils or transfected cell lines. Cells are loaded with a calcium-sensitive dye and stimulated with a CCR3 agonist like eotaxin. The antagonist's ability to inhibit the increase in intracellular calcium is measured, and the IC50 is calculated from the concentration-response curve.
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| Animal Protocol |
In vivo animal experiments for CCR3 antagonist 1 typically use models of allergic airway inflammation, such as ovalbumin (OVA)-induced asthma in mice. The compound is administered orally or intraperitoneally, and endpoints such as airway hyperresponsiveness, eosinophil infiltration in bronchoalveolar lavage fluid (BALF), and inflammatory cytokine levels are measured to assess efficacy.
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| ADME/Pharmacokinetics |
CCR3 antagonist 1 has a molecular weight of 490.42 g/mol and a high purity of ≥99.90%. It is typically stored as a powder at -20°C. It is soluble in DMSO, and stock solutions are prepared for in vitro and in vivo studies. Its stability is maintained under recommended storage conditions, with long-term storage at -20°C recommended.
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| Toxicity/Toxicokinetics |
Toxicological data for CCR3 antagonist 1 are limited to in vitro and in vivo research settings. As a potent antagonist, its safety profile is not fully characterized. However, in preclinical studies, it is typically well-tolerated at therapeutic doses. It is not approved for human use and is classified as a research chemical.
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| References | |
| Additional Infomation |
CCR3 antagonist 1 is a research compound with no clinical approval. It is a valuable tool for studying the role of the CCR3 receptor in immune function and inflammation. It is used in drug discovery programs to explore the therapeutic potential of CCR3 antagonism for treating allergic and inflammatory diseases, including asthma and atopic dermatitis.
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| Molecular Formula |
C19H21CL2N3O4S2
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|---|---|
| Molecular Weight |
490.4237
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| Exact Mass |
489.035
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| CAS # |
879399-82-3
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| PubChem CID |
11684581
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| Appearance |
Colorless to light yellow ointment
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
592
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CO[C@H](CN1CC2=CC(=C(C=C2)Cl)Cl)CNC(=O)CSC3=NC(=CS3)CC(=O)O
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| InChi Key |
QBXNXHODSIQDRT-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C19H21Cl2N3O4S2/c20-15-2-1-12(5-16(15)21)8-24-3-4-28-14(9-24)7-22-17(25)11-30-19-23-13(10-29-19)6-18(26)27/h1-2,5,10,14H,3-4,6-9,11H2,(H,22,25)(H,26,27)/t14-/m0/s1
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| Chemical Name |
2-[2-[2-[[(2S)-4-[(3,4-dichlorophenyl)methyl]morpholin-2-yl]methylamino]-2-oxoethyl]sulfanyl-1,3-thiazol-4-yl]acetic acid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~254.88 mM)
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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 | 2.0391 mL | 10.1953 mL | 20.3907 mL | |
| 5 mM | 0.4078 mL | 2.0391 mL | 4.0781 mL | |
| 10 mM | 0.2039 mL | 1.0195 mL | 2.0391 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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