| Size | Price | Stock | Qty |
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| 1mg |
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| 25mg | |||
| Other Sizes |
| Targets |
The primary target of AC-264613 is the protease-activated receptor 2 (PAR-2). PAR-2 is a G protein-coupled receptor that is activated by proteolytic cleavage of its extracellular N-terminus, exposing a tethered ligand that binds to the receptor and triggers signaling. By acting as an agonist, AC-264613 activates PAR-2, mimicking the effects of proteolytic activation and allowing the study of downstream signaling pathways.
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| ln Vitro |
Macrophages exposed to 10 μM of AC-264613 for six hours exhibit decreased IRF5 expression and considerably lower p53 protein expression [2].
In vitro, AC-264613 is a potent and selective PAR-2 agonist with a pEC₅₀ of 7.5. It suppresses interferon regulatory factor 5 and decreases interleukin-12p40. Its activity is characterized in cell-based assays measuring receptor activation and downstream signaling, such as calcium mobilization or MAP kinase phosphorylation. |
| ln Vivo |
In male Sprague-Dawley rats, AC-264613 shows a moderate elimination half-life (T1/2=2.5±2.0 h) after intraperitoneal injection (10 mg/kg) [3].
In vivo, AC-264613 has been studied for its potential in modulating inflammatory and pain signaling. By activating PAR-2, it can be used to investigate the role of this receptor in various physiological and pathological processes, including inflammation and pain. The compound's in vivo efficacy and pharmacokinetic properties have been characterized in preclinical studies. |
| Enzyme Assay |
In vitro receptor binding studies for AC-264613 measure its affinity for PAR-2. Radioligand competition assays are performed using membrane preparations from cells expressing PAR-2. The compound competes with a labeled ligand, and the affinity is determined. Selectivity over other PAR family members (PAR-1, PAR-3, PAR-4) is assessed to confirm its specificity.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Granulocyte-macrophage colony-stimulating factor (GM-CSF)-dependent macrophage Tested Concentrations: 10 μM Incubation Duration: 6 hrs (hours) Experimental Results: IRF5 expression was Dramatically diminished, and p53 protein levels were diminished. In vitro cell-based functional assays for AC-264613 evaluate its agonist activity at PAR-2. Cells expressing PAR-2 are treated with the compound, and receptor activation is measured by downstream signaling, such as calcium mobilization or MAP kinase phosphorylation. The compound's potency (pEC₅₀) and efficacy are determined from dose-response curves. |
| Animal Protocol |
In vivo animal studies for AC-264613 are conducted in models of inflammation and pain. The compound is administered via intraperitoneal or intravenous routes. Its effects on inflammatory cytokine levels and pain behavior are assessed. Pharmacodynamic studies measure PAR-2 activation in target tissues. Pharmacokinetic studies determine the compound's half-life and bioavailability.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of AC-264613 have been characterized in preclinical studies. Its molecular weight is 400.27 g/mol. For research use, it is typically stored as a powder at -20°C. Further details on its half-life, Cmax, and bioavailability are available from the primary research literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of AC-264613 has not been extensively detailed in the available literature. It is classified for research use only and not for human consumption. As a PAR-2 agonist, its potential side effects may include modulation of inflammatory responses. Standard safety precautions for handling bioactive compounds should be followed.
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| References |
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| Additional Infomation |
Additional information: AC-264613 is also known as AC264613. It is a potent and selective PAR-2 agonist with a pEC₅₀ of 7.5. The compound is used as a research tool to study PAR-2-mediated signaling in inflammation and pain. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C19H18BRN3O2
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|---|---|
| Molecular Weight |
400.276
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| Exact Mass |
399.058
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| CAS # |
1051487-82-1
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| PubChem CID |
25108278
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| Appearance |
White to off-white solid powder
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| LogP |
3.935
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
531
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C/C(=N\NC(=O)[C@H]1[C@@H](CNC1=O)C2=CC=CC=C2)/C3=CC(=CC=C3)Br
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| InChi Key |
RQKXQCSEZPQBNZ-CBCLUANDSA-N
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| InChi Code |
InChI=1S/C19H18BrN3O2/c1-12(14-8-5-9-15(20)10-14)22-23-19(25)17-16(11-21-18(17)24)13-6-3-2-4-7-13/h2-10,16-17H,11H2,1H3,(H,21,24)(H,23,25)/b22-12+/t16-,17-/m1/s1
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| Chemical Name |
(3R,4S)-rel-2-Oxo-4-phenyl-3-pyrrolidinecarboxylic acid 2-[1-(3-bromophenyl)ethylidene]hydrazide
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| Synonyms |
AC 264613 AC264613AC-264613
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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, 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4983 mL | 12.4913 mL | 24.9825 mL | |
| 5 mM | 0.4997 mL | 2.4983 mL | 4.9965 mL | |
| 10 mM | 0.2498 mL | 1.2491 mL | 2.4983 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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