| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
| Targets |
SB-328437 targets the C-C chemokine receptor 3 (CCR3), a G protein-coupled receptor that is predominantly expressed on eosinophils, basophils, and Th2 cells. CCR3 and its ligands, such as eotaxin (CCL11), eotaxin-2 (CCL24), and MCP-4 (CCL13), play a central role in the recruitment and activation of eosinophils to sites of allergic inflammation. By blocking the binding of these natural ligands to CCR3, SB-328437 hinders downstream signaling and prevents eosinophil chemotaxis.
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|---|---|
| ln Vitro |
In vitro, SB-328437 is a highly potent and selective CCR3 antagonist with an IC50 of 4 nM. It displays >2500-fold selectivity over C5aR, LTD4, CCR7, CXCR1, and CXCR2 receptors. It inhibits eotaxin-, eotaxin-2-, and MCP-4-induced calcium mobilization with IC50 values of 38, 35, and 20 nM, respectively. It also inhibits eotaxin-, eotaxin-2-, and MCP-4-induced eosinophil chemotaxis with similar potencies.
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| ln Vivo |
In vivo, SB-328437 is used to study the role of CCR3 in allergic inflammation and other eosinophil-associated diseases. Its ability to block eosinophil recruitment has been demonstrated in animal models, where it can reduce airway eosinophil infiltration and Th2-mediated inflammation. This makes it a key compound for validating CCR3 as a therapeutic target for asthma and other allergic conditions.
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| Enzyme Assay |
The inhibitory activity of SB-328437 is assessed using cell-based functional assays. Cells expressing CCR3 (e.g., RBL-2H3 cells or primary eosinophils) are treated with varying concentrations of the compound and then stimulated with CCR3 ligands such as eotaxin, eotaxin-2, or MCP-4. The reduction in intracellular calcium mobilization or cell migration is measured, and the IC50 is calculated. Receptor binding assays can also be used to assess its affinity and selectivity.
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| Cell Assay |
The cellular activity of SB-328437 is evaluated in CCR3-expressing cells, such as RBL-2H3-CCR3 cells or primary human eosinophils. Cells are treated with the compound, and its effect on ligand-induced signaling, such as calcium mobilization, is measured. Its ability to inhibit eosinophil chemotaxis is assessed using transwell migration assays. The compound's selectivity is confirmed by testing it against other chemokine receptors.
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| Animal Protocol |
In animal studies, SB-328437 is typically administered to rodents via intraperitoneal (i.p.) injection or oral gavage. In models of allergic airway inflammation, it is given to assess its effect on eosinophil infiltration into the lungs and on Th2-mediated inflammation. Disease severity is assessed by measuring inflammatory cells in bronchoalveolar lavage fluid and by histopathological examination of lung tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SB-328437 are not extensively documented in public sources. As a small molecule (MW 378.38), it is soluble in DMSO. For in vivo use, it can be formulated for oral administration or injection. Its half-life and bioavailability would need to be determined for specific applications. It is recommended to be stored at +4°C.
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| Toxicity/Toxicokinetics |
Toxicology data for SB-328437 is limited, as it is a research compound not intended for human therapeutic use. Its safety profile has not been established in formal toxicology studies. However, its potent and specific mechanism of action suggests that on-target effects related to immune modulation would be the primary concern.
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| References | |
| Additional Infomation |
SB-328437 (CAS: 247580-43-4) is a well-characterized and widely used chemical probe for studying CCR3 biology. Its high potency (IC50 = 4 nM), excellent selectivity (>2500-fold), and non-peptide nature make it an invaluable tool for investigating the role of eosinophils and CCR3 in allergic inflammation. It is a key reference compound for the development of CCR3 antagonists and continues to be used in research on asthma and other inflammatory diseases.
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| Molecular Formula |
C21H18N2O5
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|---|---|
| Molecular Weight |
378.378
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| Exact Mass |
378.122
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| CAS # |
247580-43-4
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| PubChem CID |
10474776
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| Appearance |
White to off-white solid powder
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| LogP |
4.36
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
568
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
COC(=O)[C@H](CC1=CC=C(C=C1)[N+](=O)[O-])NC(=O)C2=CC=CC3=CC=CC=C32
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| InChi Key |
VMFGCGRAIBLAFY-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C21H18N2O5/c1-28-21(25)19(13-14-9-11-16(12-10-14)23(26)27)22-20(24)18-8-4-6-15-5-2-3-7-17(15)18/h2-12,19H,13H2,1H3,(H,22,24)/t19-/m0/s1
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| Chemical Name |
methyl (2S)-2-(naphthalene-1-carbonylamino)-3-(4-nitrophenyl)propanoate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~330.36 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.50 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 20.8 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 | 2.6428 mL | 13.2142 mL | 26.4285 mL | |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2857 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 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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