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Art. -Nr.: HY-118361

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CB86

CB86 is a small-molecule ligand of the translocator protein TSPO, binding to 18-kDa TSPO with high affinity (IC₅₀ 1.6 nM). CB86 competitively binds the TSPO protein on the mitochondrial outer membrane, inhibits LPS-induced M1 pro-inflammatory activation of BV‑2 microglia, and simultaneously inhibits 6‑OHDA-induced ROS generation, apoptosis, and necrosis in PC12 cells, exerting anti-inflammatory and neuroprotective effects. CB86 can be used in research related to Parkinson's disease and rheumatoid arthritis.

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CAS. Nr.: 1150586-64-3
Formel: C₂₆H₄₃NO₃
Molecular Weight:417.63

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CB86 Chemical Structure

CAS. Nr.: 1150586-64-3

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]

TNF-α

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In Vitro

CB86 (25 μM; 24 hours) inhibits LPS-induced M1-type pro-inflammatory activation of BV-2 microglia and reduces the production of TNF-α and CD8^[2].
CB86 (25 µM; 24 h) reduces ROS fluorescence and inhibits apoptosis in 6-OHDA-induced PC12 cells^[1].
CB86 (25 µM; 24 h) protects PC12 cells against 6-OHDA-induced decreases in phase confluence/cell proliferation within 0-24 h; it inhibits induced PC12 cell necrosis, reduces LDH release, and increases cell viability^[1].
CB86 binds to TSPO in rat kidney membranes with an IC₅₀ of 1.6 nM^[2].
CB86 carries a free amino group and can be conjugated with the DTPAA-gadolinium chelator to yield the TSPO-targeted MRI contrast agent CB86-DTPA-Gd^[3].

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

Cell Proliferation Assay^[1]

Cell Line:

PC12 cells (rat adrenal pheochromocytoma)
Concentration:

25 µM
Incubation Time:

24 h
Result:

Protected PC12 cells against 6-OHDA-induced reduction in phase confluence/cell proliferation over 0-24 h.

Cell Cytotoxicity Assay^[1]

Cell Line:

PC12 cells (rat adrenal pheochromocytoma)
Concentration:

25 µM
Incubation Time:

24 h
Result:

Reduced 6-OHDA-induced LDH release in PC12 cells by 15% compared to 6-OHDA.

Cell Viability Assay^[1]

Cell Line:

PC12 cells (rat adrenal pheochromocytoma)
Concentration:

25 µM
Incubation Time:

24 h
Result:

Increased PC12 cell viability by 29.8% compared to 6-OHDA in the XTT assay.

Apoptosis Analysis^[1]

Cell Line:

PC12 cells (rat adrenal pheochromocytoma)
Concentration:

25 µM
Incubation Time:

24 h
Result:

Inhibited 6-OHDA-induced apoptosis in PC12 cells by 16% compared to 6-OHDA (1.3-fold).

ELISA Assay^[2]

Cell Line:

BV-2 murine microglial cells
Concentration:

25 μM
100 ng/mL (LPS)
Incubation Time:

24 h
Result:

Inhibited LPS-induced TNF-α levels (4.2-fold inhibition).
When applied alone, showed no effect.

Cell Viability Assay^[2]

Cell Line:

BV-2 murine microglial cells
Concentration:

25 μM
100 ng/mL (LPS)
Incubation Time:

24 h
Result:

Reduced LPS-elevated metabolism to control levels.
When applied alone, showed no effect.

Related Protocols :

Chemical Information

CAS. Nr. 1150586-64-3
Molecular Weight 417.63
Formel C₂₆H₄₃NO₃
SMILES

O=C(NC1CC1)CCCCCCCOC2=CC(O)=CC(=C2)C(C)(C)CCCCCC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Monga S, et al. The Neuro-Protective Effects of the TSPO Ligands CB86 and CB204 on 6-OHDA-Induced PC12 Cell Death as an In Vitro Model for Parkinson's Disease. Biology. 2021 Nov 15;10(11):1183.

[2]. Monga S, et al. The protective effect of the TSPO ligands 2,4-Di-Cl-MGV-1, CB86, and CB204 against LPS-induced M1 pro-inflammatory activation of microglia. Brain Behav Immun Health. 2020 May 21;5:100083.

[3]. Hou Z, et al. Gadolinium-conjugated CB86: a novel TSPO-targeting MRI contrast agent for imaging of rheumatoid arthritis. Journal of drug targeting. 2020 Apr;28(4):398-407.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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CB86

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