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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 402-40-4
- 分子式: C27H38Br2N2O
- 分子量:566.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
AChE |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 402-40-4
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分子量 566.41
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)