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Nalfurafine

  Cat. No.:  DC23102   Featured
Chemical Structure
152657-84-6
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More than 5000 active chemicals with high quality for research!
Field of application
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).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 152657-84-6
Chemical Name: 2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-
Synonyms: TRK-820;TRK820
SMILES: O=C(N(C1CCC2(C3N(CCC42C2=C(OC14)C(=CC=C2C3)O)CC1CC1)O)C)/C=C/C1C=COC=1
Formula: C28H32N2O5
M.Wt: 476.5641
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment[2].
Target: IC50: kappa opioid receptor (KOR)[1]
In Vivo: Nalfurafine (subcutaneous injection; 0.015 mg/kg) combines with EOM-salvinorin-B produces spinal antinociception equivalent to 5 mg/kg, it also enhances the supraspinal analgesic effect of 5 mg/kg morphine[1]. Nalfurafine (subcutaneous injection; 4 μg/kg) causes a dose-dependent increase of the inhibition of the acetic acid-induced abdominal constriction,and the inhibition of the abdominal constriction reaches its peak 30 min after injection, gradually declined and returned to the preinjection level 4 hr after[2]. Animal Model: Male and Female C57BL/6J mice[1] Dosage: 0.015 mg/kg Administration: Subcutaneous injection Result: Had the potential for enhancing the therapeutic potential of MOR-targeting analgesics, such as morphine.
References: [1]. Kaski SW, et al. Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine.J Pharmacol Exp Ther. 2019 Nov;371(2):487-499. [2]. Endoh T, et al. Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.Life Sci. 1999;65(16):1685-94.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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