BW284C51
BW284C51 is a highly selective Acetylcholinesterase inhibitor. BW284C51 exerts non-competitive, voltage-dependent blocking effects on the Torpedo nicotinic acetylcholine receptor channel. BW284C51 impairs acetylcholine clearance to increase acetylcholine exposure, and enhances the acetylcholine-mediated expression response of melanogenesis-related genes. BW284C51 can be used in research related to Alzheimer's disease, Parkinson's disease, congenital myasthenia, schizophrenia and familial epilepsy.
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- No. CAS: 402-40-4
- Fòrmula: C27H38Br2N2O
- Peso molecular:566.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
AChE |
In Vitro
BW284C51 acts as a potent, reversible, voltage-dependent noncompetitive antagonist of Torpedo marmorata nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes, with an IC50 of 0.5 μM for inhibition of 10 μM acetylcholine-elicited currents, and selectively targets nicotinic over muscarinic receptors[2].
BW284C51 (20 μM) enhances acetylcholine-mediated suppression of melanogenesis, including reduced melanin content, decreased CRE/MITF/TYR promoter activity, and lowered MITF and TYR protein levels, in B16F10 murine melanoma cells[3].
BW284C51 (20 μM) does not enhance muscarinic acetylcholine receptor agonist-mediated suppression of CRE and MITF promoter activity in B16F10 murine melanoma cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BW284C51 (0.2 mg/kg/day; i.p.; daily; 5 days pre-transplant) decreases marrow endothelial cells in syngeneic hematopoietic cell transplant-treated C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[1]
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Dosage:0.2 mg/kg/day
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Administration:i.p.; daily; 5 days
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Result:Increased marrow peri-arteriolar endothelial cells to 0.00396 as a proportion of stromal cells, compared to 0.00204 in controls.
Increased sinusoidal endothelial cells to 0.0814 as a proportion of stromal cells, compared to 0.0461 in controls.
Induced differential gene expression in sorted marrow endothelial cells clustered in pathways involving hematopoiesis, leukocyte activation and differentiation, inflammatory responses, and immune regulation.
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Animal Model:C57BL/6[1]
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Dosage:0.2 mg/kg/day
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Administration:i.p.; daily; 5 days pre-transplant
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Result:Decreased marrow endothelial cells post-hematopoietic cell transplant.
Chemical Information
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No. CAS 402-40-4
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Peso molecular 566.41
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Fòrmula C27H38Br2N2O
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SMILES
O=C(CCC1=CC=C([N+](C)(C)CC=C)C=C1)CCC2=CC=C([N+](C)(C)CC=C)C=C2.[Br-].[Br-]
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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)
BW284C51 Related Classifications
HY-137852 Related Classifications
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