| Size | Price | Stock | Qty |
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| 1mg |
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AZD2423 (AZD-2423) is a novel and potent negative allosteric modulator of CCR2 with the potential to be used in posttraumatic neuralgia. AZD2423 inhibited CCR2 Ca2+ flux with an IC50 of 1.2 nM. AZD2423 is an orally bioavailable non-competitive, negative allosteric modulator of the CCR2 chemokine receptor. CCR2 is a receptor for monocyte chemoattractant protein MCP-1 (CCL2) and the closely related proteins MCP-2 (CCL8), MCP-3 (CCL7), and MCP-4 (CCL13). Human CCR2 exists as two forms, CCR2a and CCR2b, which differ at their C-termini by alternative splicing. Evidence obtained from studies on leukocytes suggests that MCP-1 binds preferentially to CCR2 and mediates monocyte chemotaxis. Studies have implicated MCP-1-mediated monocyte infiltration in pain and a range of inflammatory diseases. AZD2423 has been developed for the oral treatment of neuropathic pain and chronic obstructive pulmonary disease (COPD). In pre-clinical studies, AZD2423 inhibited MCP-1 induced calcium mobilization and chemotaxis of THP-1 cell line with an IC50 of 4 nM. The AZD2423 affinity for CCR2 in human whole blood, measuring MCP-1 induced L-selectin shedding from monocytes, was the same. AZD2423 is highly selective (> 500-fold) for CCR2. AZD2423 demonstrated robust analgesia in two rodent models of neuropathic pain and a pain model of joint destruction against heat, mechanical and weight-bearing endpoints. A significant (> 500-fold) drop-off in potency was observed for several pre-clinical species (rat, mouse, dog, marmoset). Consequently several tool compounds have been used for most in vivo pharmacology studies; a tool CCR2 antagonist inhibited neuronal excitability in rat neuropathic models to heat, mechanical and electrical stimuli either via systemic administration or via administration directly to the spinal cord.
| ln Vitro |
With an IC50 of 4 nM, AZD2423 inhibits the THP-1 cell line's MCP-1-induced calcium mobilization and chemotaxis[1].
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| References |
| 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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