SIB-1553A hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SIB-1553A 是一种口服生物有效的烟碱乙酰胆碱受体 (nAChRs) 激动剂，对含有 nAChRs 的 β4 亚单位具有选择性。SIB-1553A 也是一种选择性配体神经元 nAChR 配体。SIB-1553A 是一种认知增强剂，对阿尔茨海默病和其他认知障碍的症状研究具有潜在的研究潜力。

SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.

SIB-1553A displaces the binding of [H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM.In calcium flux assays, SIB-1553A (0.1-5 μM), shows a greater selectivity for beta4-subunit containing recombinant hnAChRs (alpha2beta4, alpha3beta4 and alpha4beta4) vs. beta2-subunit containing nAChRs (alpha4beta2 and alpha3beta2) both in terms of efficacy and potency.

SIB-1553A (1-40 mg/kg; s.c.) produces dose-dependent increases in ACh levels.Animal Model:Male Sprague-Dawley rats (200-250 g)Dosage:1, 2, 4, 10, 20 and 40 mg/kg Administration:s.c.Result:Induced hippocampal ACh release.

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Cell Cycle/DNA Damage

AChR

AChR

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191611-89-9

273.82

C13H20ClNOS

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : ≥ 27.38 mg/mL (99.99 mM)

Cl.CN1CCCC1CCSc1ccc(O)cc1

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(-20℃)

With Ice Pack

≥ 2 years