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Donecopride (fumarate hydrate) Sale

(Synonyms: MR31147) 目录号 : GC47263

A 5-HT4 receptor partial agonist and AChE inhibitor

Donecopride (fumarate hydrate) Chemical Structure

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1 mg
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5 mg
¥2,552.00
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产品描述

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E (Ki = 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50 = 16 nM).1 It is selective for AChE over butyrylcholinesterase (BChE; IC50 = 3,530 nM) but does bind to 5-HT2B and sigma-2 (σ2) receptors (Ki = 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4 with an EC50 value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2

1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Chemical Properties

Cas No. N/A SDF
别名 MR31147
Canonical SMILES NC1=CC(OC)=C(C(CCC2CCN(CC3CCCCC3)CC2)=O)C=C1Cl.OC(/C=C/C(O)=O)=O.O
分子式 C22H33ClN2O2.C4H4O4 [XH2O] 分子量 509
溶解度 DMSO: 50 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
1 mM 1.9646 mL 9.8232 mL 19.6464 mL
5 mM 0.3929 mL 1.9646 mL 3.9293 mL
10 mM 0.1965 mL 0.9823 mL 1.9646 mL
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