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Cat. No.: HY-160040

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Cobitolimod

Name: Cobitolimod
Brand: MedChemExpress
SKU: HY-160040
Price: 140.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: Kappaproct; DIMS0150)

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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.

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

Purity : 97.14%
CAS No.: 1226822-98-5
Formula: C₁₈₅H₂₃₃N₇₃O₁₀₆P₁₈S₆
Molecular Weight:5925.20

Storage:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Cobitolimod Chemical Structure

CAS No.: 1226822-98-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

TLR9

All Toll-like Receptor (TLR) Isoforms :

In Vitro

Adaptive ImmunityCytokines & ChemokinesCytokines and ChemokinesInnate ImmunityImmune Tolerance & Immunosuppression

Adaptive Immunity

Cytokines & Chemokines

Cobitolimod (100 µM; 24-72 h) suppresses CD4+IL17+ T cells in ulcerative colitis specimen-derived LPMCs through an IL10-dependent mechanism^[2].

Cytokines & Chemokines

Adaptive Immunity

Cobitolimod (100 µM; 24-72 h) shifts the LPS-induced response toward IL10/FoxP3 and away from IL6/IL17 in ulcerative colitis specimen-derived LPMCs^[2].

Cytokines and Chemokines

Cobitolimod shifts cytokine expression in isolated immune cells toward decreased IL-17 and increased IL-10^[1].
Cobitolimod (1-100 µM) dose-dependently induces IL6, TGFβ, and especially IL10 in ulcerative colitis specimen-derived LPMCs^[2].

Innate Immunity

Cobitolimod (25-200 µg/mL; 60 s association and 180 s dissociation) binds TLR9 directly in a cell-free QCM assay with strong affinity and medium-fast association/fast dissociation kinetics^[2].

Innate Immunity

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Cobitolimod (100 µM) promotes IL10 production mainly by CD4+ T cells and CD14+ macrophages in ulcerative colitis specimen-derived LPMC/PBMC cultures and shifts macrophages toward a CD163+CD206+ wound-healing phenotype^[2].

Innate Immunity

Cytokines & Chemokines

Cobitolimod (1-100 µM; 48 h) induces IL10 in mouse splenocytes through TLR9 signaling^[2].
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

Adaptive ImmunityCytokines & ChemokinesImmune Tolerance & Immunosuppression

Adaptive Immunity

Cytokines & Chemokines

Cobitolimod (Rectal) ameliorates DSS (HY-116282C)-induced colitis in mice and lowers intestinal Th17/IL-17 inflammatory responses^[1].

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Cobitolimod (40-250 µg; rectal; days 4 and 8; two total administrations during the 10-day DSS protocol) ameliorates DSS-induced murine colitis and shifts mucosal immunity toward IL10/FoxP3 responses and away from IL17/Th17 responses^[2].

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

Animal Model:

Balb/c (female, 8 weeks old) injected with DSS^[2]
Dosage:

40 µg; 84 µg; 250 µg
Administration:

rectal administration; on days 4 and 8; two total administrations during the 10-day DSS protocol
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.

Related Protocols :

Chemical Information

CAS No. 1226822-98-5
Appearance Solid
Molecular Weight 5925.20
Formula C₁₈₅H₂₃₃N₇₃O₁₀₆P₁₈S₆
Color White to off-white
SMILES

[Cobitolimod]
Synonyms

Kappaproct; DIMS0150
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2242 KB)

References

[1].
M de Bruyn, et al. OP003 Temporal changes in immune pathways with consecutive biological therapies as measured by serum proteomics Get access Arrow. 16 January 2018.

[2]. Schmitt H, et al. The TLR9 Agonist Cobitolimod Induces IL10-Producing Wound Healing Macrophages and Regulatory T Cells in Ulcerative Colitis. Journal of Crohn's & colitis. 2020 May 21;14(4):508-524. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Cobitolimod

All Toll-like Receptor (TLR) Isoforms