ARC 239
Based on 2 publication(s) in Google Scholar
ARC 239 is a selective α2B/C-adrenoceptor antagonist, with pKi values of 5.45, 7.06, and 6.95 for α2A, α2B, and α2C receptors, respectively. ARC 239 selectively antagonizes α2B-AR, blocking norepinephrine signaling and downstream RhoA/ROCK activation and Claudin-5 disruption, without altering plasma norepinephrine levels in the distal tail artery of mice, and does not inhibit α2-adrenoceptor-mediated vasoconstriction. ARC 239 also binds with high affinity to 5-HT1A receptors, with a Ki of 63.1 nM, thereby interfering with subtype-selective α2-adrenoceptor assays. ARC 239 can be used for research on cardiovascular diseases and inflammatory skin diseases.
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- Pureté : 99.28%
- CAS No.: 67339-62-2
- Formule: C24H29N3O3
- Masse moléculaire:407.51
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ARC 239
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Activité biologique
Description
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5-HT1A Receptor 63.1 nM (Ki) |
human α2C-adrenoceptor 6.95 (pKi) |
Alpha-2C adrenergic receptor 7.06 (pKi) |
Alpha-2A adrenergic receptor 5.45 (pKi) |
Alpha-2B adrenergic receptor 4.6 nM (Kd) |
ROCK |
Claudin-5 |
In Vitro
ARC 239 (0.3-1 µM; 60 min) competitively antagonizes Norepinephrine (HY-13715)-induced contraction of human saphenous vein rings with a pKB of 7.19[1].
ARC 239 (0.1 nM-0.1 mM; incubated at 37°C for 30 min) recognizes rat cortical 5-HT1A receptors in a [3H]8-OH-DPAT competitive binding assay with a Ki of 63.1 nM[2].
ARC 239 (0.1 nM-0.1 mM; incubated at 25°C for 30 min) displaces the binding of [3H]RX 821002 to rat hippocampal 5-HT1A receptors under conditions where α2-adrenoceptors are masked, with a Ki of 136 nM[2].
ARC 239 dihydrochloride (30 μM; pretreatment for 30 min + co-incubation for 48 h) prevents Norepinephrine bitartrate monohydrate (HY-13715B) (5 µM)-induced RhoA activation, ROCK-dependent MYPT1 phosphorylation, and loss of Claudin-5 tight junctions in HUVECs[3].
ARC 239 (50 nM; 30 min) does not inhibit α2-AR-mediated vasoconstriction in isolated distal mouse tail arteries at 37°C or 28°C, which is consistent with its KD of 4.6 nM for α2B-AR and KD >50 nM for mouse tail arteries[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs
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Concentration:30 μM
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Incubation Time:pre-incubation 30 min + co-incubation 48 h
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Result:Prevented Norepinephrine-induced reduction of Claudin-5 protein levels and disruption of junctional localization, including fragmentation and discontinuity consistent with tight junction disassembly.
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Cell Line:HUVECs
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Concentration:30 μM
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Incubation Time:pre-incubation 30 min + co-incubation 48 h
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Result:Inhibited Norepinephrine-enhanced RhoA-GTP signaling.\nAbolished norepinephrine-induced increase in p-MYPT1/MYPT1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (7-week-old; female) were subcutaneously injected of Resiniferatoxin (RTX) for 3 consecutive days[3]
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Dosage:5 mg/kg
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Administration:i.p.; once daily; administered continuously throughout the stress exposure and psoriasis induction process
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Result:Effectively suppressed stress-induced skin vascular leakage (confirmed by a significant reduction in Evans blue dye extravasation).
Did not affect plasma norepinephrine (NE) levels in mice, indicating that it functions downstream of NE (i.e., at the receptor level).
Chemical Information
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CAS No. 67339-62-2
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Appearance Solid
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Masse moléculaire 407.51
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Formule C24H29N3O3
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Color White to off-white
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SMILES
O=C1N(CCN2CCN(C3=CC=CC=C3OC)CC2)C(C(C)(C)C4=C1C=CC=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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iScience
2026 Feb 23;29(3):115122. PMID: 41852725 -
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (122.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (292 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gavin KT, et al. Alpha 2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):406-11. [Content Brief]
[2]. Meana JJ, et al. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur J Pharmacol. 1996 Oct 3;312(3):385-8. [Content Brief]
[3]. Yu Y, et al. A stress-responsive neurovascular axis shapes skin immune accessibility. iScience. 2026 Mar 20;29(3):115122. [Content Brief]
[4]. Di Cicco E, et al. A TERRA-NONO axis drives fibroblast reprogramming in cancer. Sci Adv. 2026 Oct 2;12(40):eaed3358. [Content Brief]
[5]. Chotani MA, et al. Silent alpha(2C)-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries. Am J Physiol Heart Circ Physiol. 2000 Apr;278(4):H1075-83. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4539 mL | 12.2696 mL | 24.5393 mL | 61.3482 mL |
| 5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL | 12.2696 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4539 mL | 6.1348 mL | |
| 15 mM | 0.1636 mL | 0.8180 mL | 1.6360 mL | 4.0899 mL | |
| 20 mM | 0.1227 mL | 0.6135 mL | 1.2270 mL | 3.0674 mL | |
| 25 mM | 0.0982 mL | 0.4908 mL | 0.9816 mL | 2.4539 mL | |
| 30 mM | 0.0818 mL | 0.4090 mL | 0.8180 mL | 2.0449 mL | |
| 40 mM | 0.0613 mL | 0.3067 mL | 0.6135 mL | 1.5337 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2270 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0225 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3067 mL | 0.7669 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL |
ARC 239 Related Classifications
HY-12709 Related Classifications
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Keywords
- ARC 239
- 67339-62-2
- ARC239
- ARC-239
- Adrenergic Receptor
- 5-HT Receptor
- ROCK
- Claudin
- Beta Receptor
- Serotonin Receptor
- 5-hydroxytryptamine Receptor
- Rho-associated protein kinase
- Rho-associated kinase
- Rho-kinase
- ROK
- 5-HT1A receptor
- Claudin-5
- RhoA
- human saphenous vein
- noradrenaline
- vascular leakage
- α1-adrenoceptor
- α2-adrenoceptor
- α2B-adrenoceptor
- Inhibitor
- inhibitor
- inhibit