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Aspirin COX remmer

Cat.Nr.S3017

Aspirin is een salicylaat en een irreversibele COX1- en COX2-remmer, gebruikt als pijnstiller om kleine pijntjes te verlichten, als koortswerend middel om koorts te verminderen, en als ontstekingsremmer. Deze verbinding induceert autophagy en stimuleert mitophagy.
Aspirin COX remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 180.16

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%
99.99

Celkweek, behandeling & werkconcentratie

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving PMID
AGS Function assay 15 to 60 umol/L after 12 hrs Inhibition of Escherichia coli-stimulated IL-8 production in human AGS cells at 15 to 60 umol/L after 12 hrs by ELISA 20153183
microglia cells Antineuroinflammatory assay 15 mins Antineuroinflammatory activity in LPS-stimulated rat microglia cells assessed as inhibition of PMA-stimulated TXB2 release preincubated for 15 mins measured 70 mins after PMA challenge, IC50=3.12μM 22153874
HCT116 Function assay 1 mM 6 hrs Inhibition of TNF-alpha-induced NF-kappaB activation in human HCT116 cells at 1 mM after 6 hrs by luciferase reporter gene assay 22154834
SKBR3 Growth inhibition assay 300 uM 48 hrs Growth inhibition of human SKBR3 cells at 300 uM after 48 hrs by alamar blue assay 22494617
PANC1 Growth inhibition assay 300 uM 48 hrs Growth inhibition of human PANC1 cells at 300 uM after 48 hrs by alamar blue assay 22494617
PC3 Growth inhibition assay 300 uM 48 hrs Growth inhibition of human PC3 cells at 300 uM after 48 hrs by alamar blue assay 22494617
MDA-MB-231 Function assay 100 uM 30 mins Irreversible inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay 23651359
THP1 Function assay 100 uM 30 mins Irreversible inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay 23651359
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs MTT assay 26750401
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of IL-6 in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by ELISA 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of TNF-alpha in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs in presence of leonurine by E 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress in rat H9c2 cells assessed as antioxidant activity by measuring reduction in MDA levels at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by spectrophotometry 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress in rat H9c2 cells assessed as antioxidant activity by measuring increase in SOD activity at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by spectrophotometry 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress in rat H9c2 cells assessed as antioxidant activity by measuring increase in catalase activity at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by spectrophotometry 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of TNF-alpha in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by ELISA 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of IL-1beta in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by ELISA 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress in rat H9c2 cells assessed as reduction in MDA levels at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs in presence of leonurine by spectrophotometry 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress in rat H9c2 cells assessed as antioxidant activity by measuring increase in SOD activity at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs in presence of leonurine by spec 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of IL-6 in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs in presence of leonurine by ELISA 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced oxidative stress mediated inflammation in rat H9c2 cells assessed as suppression of IL-1beta in supernatant at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs in presence of leonurine by EL 27575471
H9c2 Cardioprotective assay 1 uM 8 hrs Cardioprotective activity against hypoxia-induced cytotoxicity in rat H9c2 cells assessed as increase in cell viability at 1 uM preincubated for 8 hrs followed by H2O2 addition for 2 hrs by MTT assay 27575471
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by measuring nitrite accumulation by Griess method, IC50=43.2μM 28561586
stem cells Function assay 100 uM 5 days Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production at 100 uM measured on day 5 in presence of IDX by ELISA 29398443
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
peritoneal cells Function assay 5 hrs Inhibition of LPS-induced PGE2 production in C57BL6 mouse peritoneal cells measured at 5 hrs time interval by ELISA, IC50=4.08μM 30006172
HCT8 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT8 cells after 72 hrs in presence of cinnamaldehyde by MTT assay, IC50=15.6μM 30037494
RPMI8226 Cell cycle assay 1.7 uM 48 hrs Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G0/G1 phase at 1.7 uM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib 30590258
RPMI8226 Cell cycle assay 1.7 uM 48 hrs Cell cycle arrest in human RPMI8226 cells assessed as accumulation at S phase at 1.7 uM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib 30590258
RPMI8226 Cell cycle assay 1.7 uM 48 hrs Cell cycle arrest in human RPMI8226 cells assessed as reduction in accumulation at G2/M phase at 1.7 uM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib 30590258
HaCaT Antipyretic assay 100 uM 2 hrs Antipyretic activity in human HaCaT cells assessed as inhibition of TNFalpha-induced PGE2 production at 100 uM pre-incubated for 2 hrs before TNFalpha stimulation for 24 hrs by ELISA 31393125
OVCAR5 Function assay 300 uM to 1 mM 72 hrs Inhibition of NAPRT in human OVCAR5 cells assessed as potentiation of NAMPT inhibitor FK866-induced cytotoxicity by measuring reduction in cell viability at 300 uM to 1 mM incubated for 72 hrs by SRB assay ChEMBL
CCRF-CEM Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human CCRF-CEM cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further ChEMBL
Jurkat Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human Jurkat cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further i ChEMBL
ML2 Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human ML2 cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further incu ChEMBL
NOMO Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human NOMO cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further inc ChEMBL
NB4 Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human NB4 cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further incu ChEMBL
NAMALWA Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human NAMALWA cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further ChEMBL
Daudi Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human Daudi cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further in ChEMBL
Raji Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human Raji cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further inc ChEMBL
ARH77 Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human ARH77 cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further in ChEMBL
RPMI8226 Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human RPMI8226 cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further ChEMBL
U266 Function assay 3.5 mM 48 hrs Inhibition of NAPRT in human U266 cells assessed as potentiation of NAMPT inhibitor FK866-induced apoptosis by measuring reduction in cell viability at 3.5 mM prer-incubated with IC50 level of FK866 for 48 hrs followed by compound addition and further inc ChEMBL
NAMALWA Function assay 35 mg/kg 45 days Potentiation of NAMPT inhibitor 10 mg/kg, ip bid FK866-induced antitumor activity in human NAMALWA cells xenografted in SCID mouse assessed as increase in mouse survival at 35 mg/kg, ip bid up to 45 days ChEMBL
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht 180.16 Formule

C9H8O4

 Opslag (Vanaf de ontvangstdatum)
CAS-nr. 50-78-2 SDF downloaden Opslag van stamoplossingen

Synoniemen NSC 27223, Acetylsalicylic acid, ASA Smiles CC(=O)OC1=CC=CC=C1C(=O)O

Oplosbaarheid

In vitro
Batch:

DMSO : 36 mg/mL (199.82 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 36 mg/mL

Water : Insoluble

Molariteitscalculator

Massa Concentratie Volume Moleculair gewicht
Verdunningscalculator Moleculair gewicht calculator

In vivo
Batch:

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC50/Ki
COX2
COX1
In vitro
Aspirin remt de activering van NF-kappa B, voorkomt zo de afbraak van de NF-kappa B-remmer, I kappa B, en daardoor blijft NF-kappa B in het cytosol. Deze verbinding remt ook NF-kappa B-afhankelijke transcriptie van de Ig kappa-enhancer en de lange terminale repeat (LTR) van het humaan immunodeficiëntievirus (HIV) in getransfecteerde T-cellen. Het en salicylaat worden gedeeltelijk gemedieerd door hun specifieke remming van IKK-beta, waardoor activering door NF-kappaB van genen die betrokken zijn bij de pathogenese van de ontstekingsreactie wordt voorkomen. Deze chemische stof is beschermend tegen neurotoxiciteit veroorzaakt door het exciterende aminozuur glutamaat in primaire neuronale culturen en hippocampale plakjes van ratten. Het activeert de transcellulaire biosynthese van een voorheen onbekende klasse eicosanoïden tijdens co-incubaties van menselijke navelstrengveneusendotheelcellen (HUVEC) en neutrofielen [polymorfonucleaire leukocyten (PMN)]. Dit middel roept een unieke klasse eicosanoïden op die worden gevormd door geacetyleerde PGHS-2- en 5-lipoxygenase-interacties. De behandeling remt de fosforylering van IRS-1 bij Ser307, evenals de fosforylering van JNK, c-Jun, en de afbraak van IkappaBalpha in 3T3-L1- en Hep G2-cellen behandeld met tumornecrosefactor (TNF)-alfa. Deze behandeling remt de fosforylering van Akt en het zoogdierdoelwit van rapamycine (maar niet de extracellulair gereguleerde kinase of PKCzeta) als reactie op TNF-alfa. Het herstelt de insuline-geïnduceerde glucoseopname in 3T3-L1-adipocyten die vooraf zijn behandeld met TNF-alfa.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/7568157/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12714600/

Toepassingen

Methoden Biomarkers Afbeeldingen PMID
Western blot MCL-1 p-AKT / AKT / p-ERK / ERK p-AMPKα / AMPKα / p-ACC / ACC SHH / SMO / GLI1 / Bcl-2 / Foxm1
S3017-WB1
26918349
Growth inhibition assay Cell proliferation Cell viability
S3017-viability1
28446712

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer Rekrutering Aandoeningen Sponsor/Medewerkers Startdatum Fasen
NCT05960864 Not yet recruiting
Ankylosing Spondylitis (AS) / Radiographic Axial SpA (r-axSpA)|Non-radiographic Axial Spondyloarthritis (Nr-axSpA)|Axial Psoriatic Arthritis (axPsA)|Acute Anterior Uveitis (AAU)|Crohn Disease (CD)|Ulcerative Colitis (UC)|Reactive Arthritis (ReA)
Southwest Hospital China
 September 2024 --
NCT05868525 Recruiting
Blunt Cerebrovascular Injury
Loma Linda University
 July 2024 Phase 4
NCT06197009 Not yet recruiting
Axial Spondyloarthritis
Sinocelltech Ltd.
 July 1 2024 Phase 2
NCT06378398 Not yet recruiting
Colorectal Neoplasia
University of Michigan Rogel Cancer Center|National Cancer Institute (NCI)
 May 2024 Early Phase 1

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