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Nalfurafine (TRK-820)

Cat. No. M21699
Nalfurafine (TRK-820) Structure
Synonym:

TRK-820

Size Price Availability Quantity
5mg USD 390  USD390 In stock
10mg USD 560  USD560 In stock
25mg USD 900  USD900 In stock
50mg USD 1150  USD1150 In stock
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Quality Control & Documentation
Biological Activity

Nalfurafine is an effective and selective agonist of G protein-biased κ-opioid receptor with high translational potential. Nalfurafine enhances the therapeutic potential of MOR-targeting analgesics.

In vivo, Nalfurafine (4 μg/kg; s.c.) increased the inhibition of the acetic acid-induced abdominal constriction in a dose-dependent manner, inhibited the abdominal constriction reaching its peak 30 min after injection, gradually declined, and returned to the preinjection level 4 hr after. Nalfurafine (0.015 mg/kg; s.c.) combines with EOM-salvinorin-B produced spinal antinociception equivalent to 5 mg/kg.

Chemical Information
Molecular Weight 476.56
Formula C28H32N2O5
CAS Number 152657-84-6
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yan Zhou, et al. Handb Exp Pharmacol. Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist

[2] Shane W Kaski, et al. J Pharmacol Exp Ther . Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine

[3] Hugh C Rayner, et al. Clin J Am Soc Nephrol. International Comparisons of Prevalence, Awareness, and Treatment of Pruritus in People on Hemodialysis

[4] Thomas Mettang, et al. Kidney Int. Uremic pruritus

[5] T Endoh, et al. Jpn J Pharmacol. TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys

[6] T Endoh, et al. Eur J Pharmacol. Characterization of the antinociceptive effects of TRK-820 in the rat

[7] T Endoh, et al. Life Sci . Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist

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