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首页 / 抑制剂/激动剂 / 神经信号通路 / AChR / nAChR agonist 1

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

货号：A1275154 Ambeed 开学季，买赠积分，赢豪礼

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 化学结构
CAS号：1394371-75-5
nAChR agonist 1 3D分子结构
CAS号：1394371-75-5
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]}
批次查询： 批次纯度:

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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

 		{[allProObj[0].p_purity_real_show]}
Loganin ++

AChE, IC50: 3.95 μM

 		{[allProObj[0].p_purity_real_show]}
topride HCl ++

AChE, IC50: 2.04 μM

 		{[allProObj[0].p_purity_real_show]}
Dehydroevodiamine HCl ✔ {[allProObj[0].p_purity_real_show]}
Jatrorrhizine ++

AChE, IC50: 872 nM

 		{[allProObj[0].p_purity_real_show]}
Palmatine ++

AChE, IC50: 0.51 μM

 		{[allProObj[0].p_purity_real_show]}
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

 		{[allProObj[0].p_purity_real_show]}
Galanthamine HBr ++

AChE, IC50: 0.35 μM

 		{[allProObj[0].p_purity_real_show]}
Trospium chloride ✔ {[allProObj[0].p_purity_real_show]}
Tiotropium Bromide Monohydrate ✔ {[allProObj[0].p_purity_real_show]}
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

 		{[allProObj[0].p_purity_real_show]}
Hexamethonium Bromide ✔ {[allProObj[0].p_purity_real_show]}
Pancuronium dibromide ✔ {[allProObj[0].p_purity_real_show]}
Neostigmine bromide ✔ {[allProObj[0].p_purity_real_show]}
Orphenadrine citrate ✔ {[allProObj[0].p_purity_real_show]}
Oxybutynin ✔ {[allProObj[0].p_purity_real_show]}
Irsogladine ✔ PDE {[allProObj[0].p_purity_real_show]}
Pyridostigmine bromide ✔ {[allProObj[0].p_purity_real_show]}
Rivastigmine +

AChR, IC50: 5.5 μM

 		{[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Rocuronium Bromide ✔ {[allProObj[0].p_purity_real_show]}
Tropicamide +++

M4 mAChR, IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Diphenmanil methylsulfate ✔ {[allProObj[0].p_purity_real_show]}
Umeclidinium bromide ✔ {[allProObj[0].p_purity_real_show]}
Otilonium bromide ✔ {[allProObj[0].p_purity_real_show]}
Flavoxate HCl +

mAChR, IC50: 12.2 μM

 		{[allProObj[0].p_purity_real_show]}
Ipratropium bromide ✔ {[allProObj[0].p_purity_real_show]}
Diphenidol HCl ✔ {[allProObj[0].p_purity_real_show]}
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

 		{[allProObj[0].p_purity_real_show]}
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

 		{[allProObj[0].p_purity_real_show]}
Oxybutynin chloride ✔ {[allProObj[0].p_purity_real_show]}
Pentoxyverine citrate ✔ {[allProObj[0].p_purity_real_show]}
Solifenacin ✔ {[allProObj[0].p_purity_real_show]}
Catharanthine ✔ {[allProObj[0].p_purity_real_show]}
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

 		{[allProObj[0].p_purity_real_show]}
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

 		{[allProObj[0].p_purity_real_show]}
PNU-120596 ++

α7 nAChR, EC50: 216 nM

 		{[allProObj[0].p_purity_real_show]}
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

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

液体 -20°C:3-6个月-80°C:12个月
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

Tags: nAChR agonist 1 | 1394371-75-5 | α7 nAChR Positive Allosteric Modulator | Membrane Transporter/Ion Channel | Neuronal Signaling | nAChR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | nAChR agonist 1 纯度/质量文件 | nAChR agonist 1 亚型比较 | 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

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