| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ARC-239 targets α2B- and α2C-adrenergic receptors. It acts as a selective antagonist with pKi values of 7.06 for rat kidney α2B and 6.95 for human α2C adrenergic receptors. It exhibits high selectivity for α2B- and α2C-adrenoceptor subtypes over α2A-adrenoceptors. ARC-239 also inhibits the 5-HT1A receptor with a Ki of 63.1 nM.
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| ln Vitro |
In vitro, ARC-239 demonstrates high affinity and selectivity for α2B- and α2C-adrenergic receptors. It has pKi values of 7.06 for rat kidney α2B and 6.95 for human α2C adrenergic receptors. ARC-239 also inhibits the 5-HT1A receptor with a Ki of 63.1 nM. These in vitro activities confirm its profile as a selective α2B/C-adrenergic receptor antagonist with additional 5-HT1A receptor affinity.
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| ln Vivo |
In vivo, ARC-239 is used as a research tool to study the physiological and pharmacological roles of α2-adrenergic receptors. Its selectivity for α2B- and α2C-subtypes makes it valuable for distinguishing the functions of different α2-adrenoceptor subtypes. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature.
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| Enzyme Assay |
The in vitro receptor binding assay for ARC-239 typically involves radioligand displacement studies using membrane preparations from tissues or cells expressing α2-adrenergic receptor subtypes. The compound's affinity (pKi) is determined by measuring its ability to displace a specific radiolabeled ligand from rat kidney α2B and human α2C receptors. Its affinity for 5-HT1A receptors is assessed similarly.
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| Cell Assay |
In vitro cellular assays for ARC-239 assess its functional antagonism at α2-adrenergic receptors. Cells expressing α2B- or α2C-adrenergic receptors are stimulated with an α2-agonist, and the compound's ability to inhibit downstream signaling is measured. These assays demonstrate the compound's functional antagonism at α2B- and α2C-adrenergic receptors in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for ARC-239 are conducted to study the physiological roles of α2-adrenergic receptor subtypes. The compound is administered to animals, and its effects on various physiological parameters are assessed. Its selectivity for α2B- and α2C-subtypes allows for the dissection of subtype-specific functions. However, specific details of these studies are not extensively detailed in the available literature.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for ARC-239 are not extensively detailed in the available literature. As a research compound, its pharmacokinetic properties such as absorption, distribution, metabolism, and excretion are not well-characterized. The compound is primarily used in in vitro and in vivo research settings. Its pharmacokinetic profile would be important for its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Specific toxicity data for ARC-239 are not extensively detailed in the available literature. As a selective α2-adrenergic receptor antagonist, its toxicity profile is likely related to its pharmacological activity. However, preclinical toxicology studies would be required to assess its safety margin. The compound is intended for research use only and is not for human use.
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| References |
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| Additional Infomation |
2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-4,4-dimethylisoquinoline-1,3-dione is a member of the piperazine class of compounds.
ARC-239 is a selective α2B/C-adrenergic receptor antagonist with pKi values of 7.06 for rat kidney α2B and 6.95 for human α2C adrenergic receptors. It also inhibits the 5-HT1A receptor with a Ki of 63.1 nM. It is a synthetic piperazine-based antagonist with selectivity for α2B- and α2C-adrenoceptor subtypes over α2A-adrenoceptors. It is a research compound used for studying adrenergic receptor pharmacology. |
| Molecular Formula |
C24H29N3O3.2[HCL]
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|---|---|
| Molecular Weight |
480.42724
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| Exact Mass |
479.174
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| CAS # |
67339-62-2
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| Related CAS # |
ARC 239 dihydrochloride;55974-42-0
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| PubChem CID |
609483
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| Appearance |
White to off-white solid powder
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| Density |
1.167g/cm3
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| Boiling Point |
595.8ºC at 760 mmHg
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| Flash Point |
314.1ºC
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| Index of Refraction |
1.576
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| LogP |
4.322
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
629
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OSEADGVOKYGIER-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N2O3/c1-25(2)20-9-5-4-8-18(20)23(28)19(24(25)29)12-13-26-14-16-27(17-15-26)21-10-6-7-11-22(21)30-3/h4-11,19H,12-17H2,1-3H3
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| Chemical Name |
2-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-4,4-dimethylnaphthalene-1,3-dione
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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 : ~50 mg/mL (~122.70 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 | 2.0815 mL | 10.4073 mL | 20.8147 mL | |
| 5 mM | 0.4163 mL | 2.0815 mL | 4.1629 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0815 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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