Cobitolimod
Based on 1 Customer Validation
Cobitolimod (DIMS0150) is a DNA oligonucleotide agonist of TLR9 agonist that activates the TLR9 signaling pathway. Cobitolimod induces the production of anti-inflammatory cytokines, balances Th17/T-reg cell responses, inhibits IL-17 expression and Th17 responses, induces IL-10 expression/production, regulatory T cells and Tr1 cells, and polarization of macrophages toward the wound-healing M2-like phenotype. Cobitolimod can be used for research on ulcerative colitis.
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- Pureté : 97.14%
- CAS No.: 1226822-98-5
- Formule: C185H233N73O106P18S6
- Masse moléculaire:5925.20
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Activité biologique
Description
IC50 & Target
[1]|
TLR9 |
In Vitro
Cobitolimod (25 µM; 8 days) biases ulcerative colitis specimen-derived CD14+ monocyte-derived macrophages toward an IL10-producing CD163+CD206+ wound-healing phenotype and reduces CD80+ pro-inflammatory macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 8 weeks old) injected with DSS[2]
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Dosage:40 µg; 84 µg; 250 µg
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Administration:rectal administration; on days 4 and 8; two total administrations during the 10-day DSS protocol
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Result:Reduced DSS-induced body-weight loss and reduced DAI compared with placebo-treated mice from day 6 through the end of the experiment.
All dose groups showed diminished endoscopic signs of inflammation by MEICS.
Reduced the histopathological score, with greater suppression in the 84 µg and 250 µg groups than in the 40 µg group.
Microarray analysis of LPMCs from DSS mice showed downregulation of pro-inflammatory genes, upregulation of IL10 signalling, and downregulation of IL17 signalling.
Flow cytometry of colonic LPMCs showed reduced RorγT+IL17+, RorγT+, and IL17+ T cells, with no observed differences in Th1 or Th2 cells and their associated transcription factors T-bet and GATA3.
Colonic qRT-PCR showed reduced IL6, IL17F, and IL17A mRNA and increased FoxP3 mRNA; no difference was observed for IL10 mRNA.
Immunofluorescence of day 10 colon showed decreased IL17+ cells and increased IL10+ and FoxP3+ cells.
Chemical Information
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CAS No. 1226822-98-5
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Appearance Solid
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Masse moléculaire 5925.20
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Formule C185H233N73O106P18S6
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Color White to off-white
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SMILES
[Cobitolimod]
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Synonyms
Kappaproct; DIMS0150
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2242 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)