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nAChR agonist 1

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Chemical Structure| 1394371-75-5 同义名 : -
CAS号 : 1394371-75-5
货号 : A1275154
分子式 : C20H18ClNO3S2
纯度 : 99%+
分子量 : 419.945
MDL号 : MFCD32671353
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：
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].
实验方案
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
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