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Nalfurafine

Chemical Structure : Nalfurafine

CAS No.: 152657-84-6

Nalfurafine (TRK-820;TRK820)

Catalog No.: PC-43172Not 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 476.5641
Formula C28H32N2O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-

References

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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