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Chemical Structure : PN6047
Catalog No.: PC-49002Not For Human Use, Lab Use Only.
PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.
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PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.
PN6047 elicited a concentration-dependent activation of Gαi G proteins in cells expressing the human δ opioid receptor with EC50 of 13.5 nM, with no effect on Gαi activation in cells expressing either the rat µ opioid receptor or human κ opioid receptors.
PN6047 (1, 3, 10 mg/kg, p.o.) is an effective antihyperalgesic in the mouse MIA model of osteoarthritis but not in the carrageenan model of acute inflammatory pain.
PN6047 does not appear to have proconvulsive activity or induce analgesic tolerance.
| M.Wt | 460.596 | |
| Formula | C26H28N4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Alexandra E Conibear, et al. J Pharmacol Exp Ther. 2020 Feb;372(2):224-236.
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