nAChR agonist 1 | α7 nAChR Positive Allosteric Modulator

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nAChR agonist 1 {[allProObj[0].p_purity_real_show]}

货号：A1275154

nAChR agonist 1 is a novel positive allosteric modulator of α7 nAChR. It has shown excellent safety profile in phase 1 clinical trials and is being evaluated for efficacy and safety as monotherapy in patients with mild to moderate Alzheimer’s disease.

nAChR agonist 1 化学结构
CAS号：1394371-75-5

nAChR agonist 1 3D分子结构
CAS号：1394371-75-5

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nAChR agonist 1 纯度/质量文件产品仅供科研

货号：A1275154 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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AChR 亚型比较

产品名称	AChE ↓ ↑	AChR ↓ ↑	mAChR ↓ ↑	nAChR ↓ ↑	其他靶点	纯度
Donepezil	+++ hAChE, IC50: 11.6 nM bAChE, IC50: 8.12 nM					98%
Loganin	++ AChE, IC50: 3.95 μM					99%+
topride HCl	++ AChE, IC50: 2.04 μM					98%
Dehydroevodiamine HCl	✔					99%+
Jatrorrhizine	++ AChE, IC50: 872 nM					99%+
Palmatine	++ AChE, IC50: 0.51 μM					98%
(-)-Huperzine A	++++ AChE (G4 form), Ki: 7 nM					98%
Galanthamine HBr	++ AChE, IC50: 0.35 μM					98%
Trospium chloride		✔				99%
Tiotropium Bromide Monohydrate		✔				98+%
Gallamine Triethiodide		+ AChR, IC50: 68.0 μM				98%
Hexamethonium Bromide		✔				99%
Pancuronium dibromide		✔				98%
Neostigmine bromide		✔				98%
Orphenadrine citrate		✔				98%
Oxybutynin		✔				98%
Irsogladine		✔			PDE	98%
Pyridostigmine bromide		✔				99+%
Rivastigmine		+ AChR, IC50: 5.5 μM				98%
Paroxetine hydrochloride		✔				97%
Rocuronium Bromide		✔				98%
Tropicamide			+++ M4 mAChR, IC50: 8 nM			98%
Diphenmanil methylsulfate			✔			98%
Umeclidinium bromide			✔			95%
Otilonium bromide			✔			98%
Flavoxate HCl			+ mAChR, IC50: 12.2 μM			98%
Ipratropium bromide			✔			98%
Diphenidol HCl			✔			98%
Darifenacin hydrobromide			++++ M3 mAChR, pKi: 8.9			98%
Aclidinium Bromide			++++ M4 mAChR, Ki: 0.21 nM M2 mAChR, Ki: 0.1 nM			98%
Oxybutynin chloride			✔			99%
Pentoxyverine citrate			✔			98%
Solifenacin			✔			98%
Catharanthine				✔		98%
Benzethonium chloride				+++ α7 nAChRs, IC50: 122 nM α4β2 nAChRs, IC50: 49 nM		99+%
Vinblastine sulfate				+ nAChR, IC50: 8.9 μM		99%
PNU-120596				++ α7 nAChR, EC50: 216 nM		99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

nAChR agonist 1 生物活性

描述

The α7 nicotinic acetylcholine receptor (α7 nAChR) is a subtype of nAChRs that plays a key role in the pathophysiology of neuropsychiatric diseases. nAChR agonist 1, also known as DUN71755, is a potent, orally bioavailable, and brain-permeable, allosteric α7 nAChR agonist. The EC50 value of nAChR agonist 1 is 0.32 µM in a Ca²⁺ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells expressing α7 nAChR. The oral bioavailability of nAChR agonist 1 in rats was 74%. nAChR agonist 1 showed excellent brain availability and brain residence time in rats. nAChR agonist 1 at 30 mg/kg had no significant CNS liabilities in locomotor activity, motor coordination, and MES/PTZ-induced seizure tests in rats^[1].

nAChR agonist 1 参考文献

[1]Sinha N, Karche NP, Verma MK, Walunj SS, Nigade PB, Jana G, Kurhade SP, Hajare AK, Tilekar AR, Jadhav GR, Thube BR, Shaikh JS, Balgude S, Singh LB, Mahimane V, Adurkar SK, Hatnapure G, Raje F, Bhosale Y, Bhanage D, Sachchidanand S, Dixit R, Gupta R, Bokare AM, Dandekar M, Bharne A, Chatterjee M, Desai S, Koul S, Modi D, Mehta M, Patil V, Singh M, Gundu J, Goel RN, Shah C, Sharma S, Bakhle D, Kamboj RK, Palle VP. Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization. J Med Chem. 2020 Feb 13;63(3):944-960. doi: 10.1021/acs.jmedchem.9b01569

nAChR agonist 1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.81mL

4.76mL

2.38mL

nAChR agonist 1 技术信息

CAS号	1394371-75-5
分子式	C₂₀H₁₈ClNO₃S₂
分子量	419.945

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 120 mg/mL(285.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

nAChR agonist 1 {[allProObj[0].p_purity_real_show]}

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nAChR agonist 1 {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

nAChR agonist 1 质控信息

nAChR agonist 1 生物活性

nAChR agonist 1 参考文献

nAChR agonist 1 实验方案

nAChR agonist 1 技术信息

最近浏览的产品

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总药量计算器

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nAChR agonist 1 纯度/质量文件产品仅供科研