2269511-95-5
Chemical Structure
Anrikefon
Synonym(s): HSK21542
- CAS No.: 2269511-95-5
- Formula:C39H57N7O5
- Molecular Weight:703.91
IUPAC Name: 6-cyano-5-(trifluoromethyl)nicotinic acid
InChIKey: VWXDZAZSCZVCPV-YFRBGRBWSA-N
SMILES: CC(N1CC2(CCN(CC2)C([C@@H](CCCCN)NC([C@@H](CC(C)C)NC([C@H](NC([C@H](N)CC3=CC=CC=C3)=O)CC4=CC=CC=C4)=O)=O)=O)C1)=O
Biological Activity: Anrikefon is a peripherally restricted kappa opioid receptor (KOR) agonist, with an IC50 of 0.54 nM, an EC50 of 2.41 pM, and a Ka of 0.068 nM against human KOR, and it exhibits high selectivity over μ and δ opioid receptors. Anrikefon exerts analgesic effects by inhibiting behaviors associated with inflammatory, postoperative and neuropathic pain, and also exerts antipruritic effects by reducing itch-related behaviors. Anrikefon can be used in research on pain, pruritus, and pruritus associated with chronic kidney disease[1][2].
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Anrikefon | Anrikefon is a peripherally restricted kappa opioid receptor (KOR) agonist, with an IC50 of 0.54 nM, an EC50 of 2.41 pM, and a Ka of 0.068 nM against human KOR, and it exhibits high selectivity over μ and δ opioid receptors. Anrikefon exerts analgesic effects by inhibiting behaviors associated with inflammatory, postoperative and neuropathic pain, and also exerts antipruritic effects by reducing itch-related behaviors. Anrikefon can be used in research on pain, pruritus, and pruritus associated with chronic kidney disease. | |||||||||||||||||||||
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References
- [1]. Wang X, et al. Antinociceptive and Antipruritic Effects of HSK21542, a Peripherally-Restricted Kappa Opioid Receptor Agonist, in Animal Models of Pain and Itch. Front Pharmacol. 2021;12:773204. Published 2021 Nov 16. [Content Brief]
- [2]. Gou X, et al. Reproductive and developmental toxicity assessment of HSK21542, a novel peripherally-restricted kappa opioid receptor agonist in rats and rabbits. Regul Toxicol Pharmacol. 2025;159:105811. [Content Brief]
