[CAS NO. 103-90-2]  Acetaminophen

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PRODUCTS SPECIFICATIONS [103-90-2]

Catalog
HY-66005
Brand
MCE
CAS
103-90-2

DESCRIPTION [103-90-2]

Overview

MDL-
Molecular Weight151.16
Molecular FormulaC8H9NO2
SMILESO=C(C)NC1=CC=C(O)C=C1

For research use only. We do not sell to patients.


Summary

Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 ( COX-2 ) inhibitor with an IC 50 of 25.8 μM; is a widely used antipyretic and analgesic agent [1] [2] [3] . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4] .


IC50 & Target

COX-2

25.8 μM (IC 50 )

COX-1

113.7 μM (IC 50 )


In Vitro

In vitro , acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC 50 113.7 μM for COX-1; IC 50 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC 50 for COX-2 for at least 5 h postadministration. Ex vivo IC 50 values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its in vitro IC 50 values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved [1] . MTT assay shows that Acetaminophen (APAP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Administering Acetaminophen (250 mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500 mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%) [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT03368664 Genzyme, a Sanofi Company|Sanofi
Multiple Sclerosis
October 24, 2017 Phase 3
NCT03145467 Pamukkale University
Acute Migraine Headache
January 2016 Phase 4
NCT05523102 Indonesia University|Dr Cipto Mangunkusumo General Hospital
Pain, Postoperative
March 31, 2022 Phase 4

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years

* The compound is unstable in solutions, freshly prepared is recommended.


Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 1653.88 mM ; Need ultrasonic)

H 2 O : 10 mg/mL ( 66.16 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.6155 mL 33.0775 mL 66.1551 mL
5 mM 1.3231 mL 6.6155 mL 13.2310 mL
10 mM 0.6616 mL 3.3078 mL 6.6155 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 0.5% CMC-Na /saline water

    Solubility: 10 mg/mL (66.16 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one: saline >> 0.5% Tween-80

    Solubility: 10 mg/mL (66.16 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one: PBS

    Solubility: 6.67 mg/mL (44.13 mM); Clear solution; Need ultrasonic

  • 4.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

  • 5.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

  • 6.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Acetamide, N-(4-hydroxyphenyl)-
Acetanilide, 4′-hydroxy-
N-(4-Hydroxyphenyl)acetamide
Acetagesic
p-Acetamidophenol
4-Acetamidophenol
Acetaminophen
N-Acetyl-p-aminophenol
Alvedon
Amadil
Anelix
Apamide
Calpol
Clixodyne
Eneril
Febro-Gesic
Febrolin
Fendon
4′-Hydroxyacetanilide
p-Hydroxyacetanilide
Lestemp
Liquagesic
Lonarid
Lyteca
Lyteca Syrup
Multin
NAPA
NAPAP
Nobedon
Panadol
Paracetamol
Tabalgin
Tempra
Tralgon
Paralen
Tylenol
Valgesic
APAP
Pyrinazine
4-Hydroxyacetanilide
4-(Acetylamino)phenol
N-Acetyl-4-aminophenol
p-(Acetylamino)phenol
Dymadon
Naprinol
Panets
Homoolan
Febrilix
Abensanil
Anaflon
Hedex
Pacemo
Parmol
Acamol
Bickie-mol
Dial-a-gesic
Temlo
Valadol
Cetadol
Acetalgin
Finimal
Dirox
Paracetamole
Ben-u-ron
Apamid
Acetaminofen
Phendon
Pedric
Napafen
Tempanal
Algotropyl
4-Acetaminophenol
Paracetamol DC
Acenol
Acenol (pharmaceutical)
N-Acetyl-4-hydroxyaniline
Biocetamol
Duorol
Crocin
NAPA (analgesic)
Fepanil
4-(N-Acetylamino)phenol
p-Acetoaminophen
Gattaphen T
Panodil
Pinex
Pinex (pharmaceutical)
Tachipirina
Paramol
Efferalgan
Citramon P
Daphalgan
Gelocatil
Resprin
Vick Pyrena
Pamol
Panadol Extend
Exdol
Ortensan
Pacemol
Anhiba
Alpiny
Paraspen
Dolprone
Paldesic
Datril
Banesin
Enelfa
Eu-Med
Tapar
Nebs
Doliprane
Febrilex
Dafalgan
Panaleve
Claratal
Momentum
Korum
Salzone
p-Aceaminophenol
Pasolind N
Disprol
Captin
Phenaphen
Parelan
Panasorb
Prodafalgan
Resfenol
NSC 109028
NSC 3991
Rhodapop NCR
Panadol Actifast
Perfalgan
Endophy
Puerxitong
Jin Gang
Daga
Sara
panadeine
Minoset
Minoset Plus
Vermidon
TylolHot
Gutte Enteric
Parageniol
Pyral
Adol
Colimex tabs
Cyclopam
Aminofen
Para-Tabs
Paracip
Dolo
Rapidol
Sanador
N-(p-Hydroxyphenyl)acetamide
Dolo 650
Femol
Tyfy
Paracet
N-(4-Hydroxyphenyl)ethanamide
Pyril
Pyretinol
Pacimol
Compap L
Pyridol
Eperimol
Huangnamin
Tamol (pharmaceutical)
Aphlogis
Paraceta