67339-62-2
Chemical Structure
ARC 239
- CAS No.: 67339-62-2
- Formula:C24H29N3O3
- Molecular Weight:407.51
IUPAC Name: 2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethylisoquinoline-1,3(2H,4H)-dione
InChIKey: JFNKXGOEOQCXDM-UHFFFAOYSA-N
SMILES: O=C1N(CCN2CCN(C3=CC=CC=C3OC)CC2)C(C(C)(C)C4=C1C=CC=C4)=O
Biological Activity: 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[1][2][3][4][5].
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ARC 239 | 99.28% | 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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ARC 239 (Standard) | ≥98% | ARC 239 Standard is the analytical standard of ARC 239 (HY-12709). This product is intended for research and analytical applications. 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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References
- [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]
