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Nalfurafine

Product Name
Nalfurafine
CAS No.
152658-17-8
Chemical Name
Nalfurafine
Synonyms
AC820;AC-820;AC 820;MT9938;MT 9938;MT-9938;Nalfurafina;TRK-820 HYDROCHLORIDE;Nafurarphine Hydrochloride;17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride
CBNumber
CB72502851
Molecular Formula
C28H33ClN2O5
Formula Weight
513.02502
MOL File
152658-17-8.mol
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Nalfurafine Property

Melting point:
207-217 °C
storage temp. 
Store at -20°C
solubility 
DMF: 16 mg/mL; DMSO: 33 mg/mL; Ethanol: 0.33 mg/mL; PBS (pH 7.2): 5 mg/mL
form 
A solid
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H336May cause drowsiness or dizziness

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P330Rinse mouth.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-4410
Product name
Nalfurafine(hydrochloride)
Purity
99.93%
Packaging
5mg
Price
$432
Updated
2021/12/16
ChemScene
Product number
CS-4410
Product name
Nalfurafine(hydrochloride)
Purity
99.93%
Packaging
10mg
Price
$780
Updated
2021/12/16
ChemScene
Product number
CS-4410
Product name
Nalfurafine(hydrochloride)
Purity
99.93%
Packaging
50mg
Price
$2160
Updated
2021/12/16
DC Chemicals
Product number
DC23132
Product name
Nalfurafinehydrochloride
Purity
>98%
Packaging
250mg
Price
$1400
Updated
2021/12/16
DC Chemicals
Product number
DC23132
Product name
Nalfurafinehydrochloride
Purity
>98%
Packaging
100mg
Price
$700
Updated
2021/12/16
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Nalfurafine Chemical Properties,Usage,Production

Description

Pruritus (chronic itching) is a common symptom seen in 25-90% of uremic patients, especially those with chronic renal failure requiring hemodialysis. Nalfurafine hydrochloride is a new member of this class that exhibits an improved safety profile as compared with its predecessors in preclinical studies. It is a potent agonist for the κ-opioid receptor (Ki = 0.24 nM, EC50 = 0.008 nM, Imax = 91%), with substantially lower binding and agonism of the - or d-opioid receptors (Ki = 2.24 and 484 nM, EC50 = 1.66 and 21.3 nM, Imax = 53 and 78%, respectively). In vivo, nalfurafine hydrochloride demonstrates potent antipruritic activity against histamine-sensitive as well as histamine-resistant itch in mouse pruritogen-induced scratching models.
The most common adverse event associated with nalfurafine hydrochloride was insomnia or sleep disturbance, seen in 10% of the treated patients. Nalfurafine is structurally related to naltrexone (Revia ), an opioid receptor antagonist marketed for treating alcohol dependence. Nalfurafine is synthesized in two steps starting from naltrexone, via reductive amination with methylamine under catalytic hydrogenation conditions, and subsequent acylation with 3(E)-(3-furyl) acryloyl chloride.

Originator

Toray industries (Japan)

Uses

Nalfurafine hydrochloride was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by hemodialysis. It showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. A new therapeutic agent for the treatment of uremic pruritus in hemodialysis patients.

brand name

Remitch

Nalfurafine Preparation Products And Raw materials

Raw materials

Preparation Products

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Nalfurafine Suppliers

Canada 1 China 56 France 1 India 2 United Kingdom 1 United States 7 Global 68
Sequoia Research Products Ltd.
Tel
--
Fax
--
Email
sales@seqchem.com
Country
United Kingdom
ProdList
3113
Advantage
69
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View Lastest Price from Nalfurafine manufacturers

Career Henan Chemical Co
Product
Nalfurafine hydrochloride 152658-17-8
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
1ton
Release date
2020-01-10

152658-17-8, NalfurafineRelated Search:

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  • TRK-820 HYDROCHLORIDE
  • (E)-N-((4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-(furan-3-yl)-N-methylacrylamide
  • 17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride
  • 2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,hydrochloride (1:1), (2E)-
  • Nafurarphine Hydrochloride
  • Nalfurafina
  • AC 820
  • AC820
  • AC-820
  • MT 9938
  • MT9938
  • MT-9938
  • 152658-17-8
  • C28H33ClN2O5
  • C28H32N2O5HCl
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  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Neurochemicals
  • Pharmaceuticals
  • Inhibitors