|4-(5-(4-氯苯基)-4-甲基-2-丙酰基噻吩-3-基)苯磺酰胺|CsnPharm

CAS No.: 1394371-75-5

nAChR agonist 1 Catalog No. CSN26128

Synonyms: DUN-71755

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.

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400-920-2911

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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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3813 mL
- 11.9063 mL
- 23.8127 mL
- 5 mM
- 0.4763 mL
- 2.3813 mL
- 4.7625 mL
- 10 mM
- 0.2381 mL
- 1.1906 mL
- 2.3813 mL

技术信息

CAS号	1394371-75-5	储存条件	粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H18ClNO3S2	运输	蓝冰
分子量	419.94	别名	DUN-71755

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nAChR agonist 1 Catalog No. CSN26128

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