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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- No. CAS: 1150586-64-3
- Fòrmula: C26H43NO3
- Peso molecular:417.63
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
TNF-α |
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.
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Cell Line:PC12 cells (rat adrenal pheochromocytoma)
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Concentration:25 µM
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Incubation Time:24 h
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Result:Protected PC12 cells against 6-OHDA-induced reduction in phase confluence/cell proliferation over 0-24 h.
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Cell Line:PC12 cells (rat adrenal pheochromocytoma)
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Concentration:25 µM
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Incubation Time:24 h
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Result:Reduced 6-OHDA-induced LDH release in PC12 cells by 15% compared to 6-OHDA.
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Cell Line:PC12 cells (rat adrenal pheochromocytoma)
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Concentration:25 µM
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Incubation Time:24 h
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Result:Increased PC12 cell viability by 29.8% compared to 6-OHDA in the XTT assay.
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Cell Line:PC12 cells (rat adrenal pheochromocytoma)
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Concentration:25 µM
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Incubation Time:24 h
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Result:Inhibited 6-OHDA-induced apoptosis in PC12 cells by 16% compared to 6-OHDA (1.3-fold).
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Cell Line:BV-2 murine microglial cells
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Concentration:25 μM
100 ng/mL (LPS) -
Incubation Time:24 h
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Result:Inhibited LPS-induced TNF-α levels (4.2-fold inhibition).
When applied alone, showed no effect.
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Cell Line:BV-2 murine microglial cells
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Concentration:25 μM
100 ng/mL (LPS) -
Incubation Time:24 h
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Result:Reduced LPS-elevated metabolism to control levels.
When applied alone, showed no effect.
- Phagocytosis Functional Assay
- Collagen-Induced Arthritis
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Human pluripotent stem cell midbrain dopaminergic neuron differentiation
- Apoptosis Solutions
- Research Protocol for Inflammation-related Diseases
Chemical Information
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No. CAS 1150586-64-3
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Peso molecular 417.63
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Fòrmula C26H43NO3
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SMILES
O=C(NC1CC1)CCCCCCCOC2=CC(O)=CC(=C2)C(C)(C)CCCCCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CB86 Related Classifications
HY-118361 Related Classifications
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