| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
AZD2423 targets the C-C chemokine receptor type 2 (CCR2). It acts as a non-competitive negative allosteric modulator (NAM), meaning it binds to an allosteric site on the receptor rather than the orthosteric binding site. It has an IC50 of 1.2 nM for CCR2 Ca2+ flux.
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| ln Vitro |
With an IC50 of 4 nM, AZD2423 inhibits the THP-1 cell line's MCP-1-induced calcium mobilization and chemotaxis[1].
In vitro, AZD2423 potently inhibits CCR2-mediated calcium flux with an IC50 of 1.2 nM. It is a selective CCR2 negative allosteric modulator. It shows high potency in CCR2 functional assays. Detailed in vitro activity data including selectivity over other chemokine receptors are available in the primary literature. |
| ln Vivo |
In vivo, AZD2423 is orally bioavailable. It has been studied in animal models of inflammatory diseases where CCR2-mediated monocyte recruitment plays a role. By modulating CCR2 activity, it reduces inflammation. Detailed in vivo efficacy data are available in preclinical literature. It is a research tool for studying CCR2 biology.
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| Enzyme Assay |
In vitro binding assays for AZD2423 typically involve evaluating its affinity for CCR2 using radioligand binding or calcium flux assays. Cells expressing CCR2 are treated with varying concentrations of the compound and stimulated with a CCR2 agonist (e.g., CCL2). Calcium mobilization is measured using fluorescent indicators. IC50 values are calculated from dose-response curves. Allosteric modulation is confirmed by Schild analysis.
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| Cell Assay |
Cell-based assays for AZD2423 involve culturing cells expressing human CCR2 (e.g., THP-1 cells or transfected cell lines). Cells are treated with AZD2423 at concentrations ranging from 0.01 nM to 10 µM. Calcium mobilization is measured using fluorescent indicators. Chemotaxis is assessed using transwell migration assays toward CCL2. Selectivity is assessed by screening against other chemokine receptors.
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| Animal Protocol |
In vivo animal experiments for AZD2423 typically involve administration to rodent models of inflammatory disease via oral gavage. Monocyte/macrophage infiltration is assessed by flow cytometry or immunohistochemistry. Inflammatory markers are measured. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Toxicity is assessed by monitoring body weight and organ histology.
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| ADME/Pharmacokinetics |
AZD2423 (molecular weight 425.93, formula C20H29ClFN5O2) is orally bioavailable. It is soluble in DMSO. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Its favorable oral bioavailability supports its use in in vivo studies.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for AZD2423 from the search results. As a CCR2 modulator, potential toxicity may include effects on immune function. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted in preclinical development. The compound is for research use only.
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| References | |
| Additional Infomation |
AZD2423 (CAS#: 1229603-37-5) is a potent, selective, orally bioavailable, non-competitive CCR2 negative allosteric modulator with an IC50 of 1.2 nM for CCR2 Ca2+ flux. It is used as a research tool for studying CCR2-mediated inflammation. Molecular weight: 425.93, formula: C20H29ClFN5O2.
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| Molecular Formula |
C20H29CLFN5O2
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|---|---|
| Molecular Weight |
425.927966833115
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| Exact Mass |
425.199
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| CAS # |
1229603-37-5
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| PubChem CID |
46213922
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
594
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1C=CC(=CC=1F)NC(N1CCN(CC1)C([C@H]1CN(CCN1)C(C)(C)C)=O)=O
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| InChi Key |
SRWQVWAIVQXPJY-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C20H29ClFN5O2/c1-20(2,3)27-7-6-23-17(13-27)18(28)25-8-10-26(11-9-25)19(29)24-14-4-5-15(21)16(22)12-14/h4-5,12,17,23H,6-11,13H2,1-3H3,(H,24,29)/t17-/m1/s1
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| Chemical Name |
4-[(2R)-4-tert-butylpiperazine-2-carbonyl]-N-(4-chloro-3-fluorophenyl)piperazine-1-carboxamide
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| Synonyms |
AZD-2423 AZD2423 AZD 2423
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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 : ~100 mg/mL (~234.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.87 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 (5.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3478 mL | 11.7390 mL | 23.4780 mL | |
| 5 mM | 0.4696 mL | 2.3478 mL | 4.6956 mL | |
| 10 mM | 0.2348 mL | 1.1739 mL | 2.3478 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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