Chemical Structure : Nalfurafine hydrochloride
CAS No.: 152658-17-8
Catalog No.: PC-43173Not For Human Use, Lab Use Only.
Nalfurafine (TRK-820, TRK820) is potent, selective agonist of kappa-opioid receptor with Ki of 3.5 nM, 15-fold less potent for μOR and little affinity for δOR (Ki=53 and 1,200 nM, respectively).
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Nalfurafine (TRK-820, TRK820) is potent, selective agonist of kappa-opioid receptor with Ki of 3.5 nM, 15-fold less potent for μOR and little affinity for δOR (Ki=53 and 1,200 nM, respectively); also potently binds to mutant κ(E297K), μ(K303E), κ(E297W) and κ(E297A) with Ki of 10-50 nM; inhibits forskolin-stimulated intracellular cAMP accumulation with IC50 of 0.15 nM, which is 100 fold smaller than that of U69593; produces potent antinociceptive effects in vivo.
Other Indication
Approved
M.Wt | 513.025 | |
Formula | C28H33ClN2O5 | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: 21 mg/mL |
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Chemical Name/SMILES |
2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, hydrochloride (1:1), (2E)- |
1. Nagase H, et al. Chem Pharm Bull (Tokyo). 1998 Feb;46(2):366-9.
2. Seki T, et al. Eur J Pharmacol. 1999 Jul 2;376(1-2):159-67.
3. Endoh T, et al. Life Sci. 1999;65(16):1685-94.
4. Endoh T, et al. Eur J Pharmacol. 2000 Jan 10;387(2):133-40.
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