ASP0819 | KCa3.1 opener | Probechem Biochemicals

Chemical Structure : ASP0819

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ASP0819 (ASP-0819, ASP 0819)

货号: PC-22574Not For Human Use, Lab Use Only.

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250 mg		Get quote

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生物&药学活性

ASP0819 is a potent, selective and orally active intermediate conductance channel KCa3.1 (IK1) opener with EC50 and Emax values of 102.4 nM and 99.0%, and 392.9 nM and 102.4% in human and rat KCa3.1-expressing cells, respectively.
ASP0819 does not show show more than 50% activity in the rKCa2.2 assay, hKCa1.1 assay, and L-type Ca2+ channel assay.
ASP0819 at doses of 0.1, 0.3, and 1 mg·kg−1 significantly recovered the decrease in muscle pressure threshold in rat fibromyalgia models of reserpine-induced myalgia (RIM) and vagotomy-induced myalgia (VIM).
ASP0819 significantly reduced both the spontaneous activity and mechanically evoked responses in Aδ-fibers in the rat RIM model.
ASP0819 significantly reduced the number of abdominal contractions as an indicator of abdominal pain behaviors in the rat visceral extension model and withdrawal responses in the osteoarthritis model, respectively.

物理化学性质&存储条件

分子量	471.01
分子式	C25H27ClN2O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-5-(6-chloro-2-methylbenzo[b]thiophen-3-yl)-2-(2-((cyclobutylamino)methyl)morpholino)benzoic acid

参考文献

1. Takeshita N, et al. J Pain Res. 2021 Jan 12;14:23-34. doi: 10.2147/JPR.S274563.

2. Arnold LM, et al. J Pain Res. 2020 Dec 10;13:3355-3369.

ASP0819 (ASP-0819, ASP 0819)

生物&药学活性

物理化学性质&存储条件

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ASP0819 (ASP-0819, ASP 0819)

生物&药学活性

物理化学性质&存储条件

参考文献

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