产品
编 号：F149438
分子式：C20H18ClNO3S2
分子量：419.94
分子式：C20H18ClNO3S2
分子量：419.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1394371-75-5
产品详情
生物活性：
nAChR agonist 1 is a potent,?brain-permeable, and?orally?efficacious positive?allosteric?modulator?of α7?nicotinic?acetylcholine?receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 μM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
体内研究：
Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial.nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively.Animal Model:Male BALB/c mice
Dosage:10 mg/kg
Administration:p.o.(Pharmacokinetic?Analysis)
Result:The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.
nAChR agonist 1 is a potent,?brain-permeable, and?orally?efficacious positive?allosteric?modulator?of α7?nicotinic?acetylcholine?receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 μM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
体内研究：
Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial.nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively.Animal Model:Male BALB/c mice
Dosage:10 mg/kg
Administration:p.o.(Pharmacokinetic?Analysis)
Result:The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.
产品资料
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