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SEN12333 {[allProObj[0].p_purity_real_show]}

货号:A1169631 同义名: WAY-317538

SEN12333是一种选择性 α7 烟碱型乙酰胆碱受体(nAChR)激动剂,对大鼠的 EC50 和 Ki 值分别为 1.6 μM 和 260 nM,同时在组胺 H3 受体上具有功能性拮抗作用(IC50 = 103 nM)。

SEN12333 化学结构 CAS号:874450-44-9
SEN12333 化学结构
CAS号:874450-44-9
SEN12333 3D分子结构
CAS号:874450-44-9
SEN12333 化学结构 CAS号:874450-44-9
SEN12333 3D分子结构 CAS号:874450-44-9
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SEN12333 纯度/质量文件 产品仅供科研

货号:A1169631 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 99%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 99%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 99%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

99%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α7 nAChRs, IC50: 122 nM

α4β2 nAChRs, IC50: 49 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 99%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

SEN12333 生物活性

描述 SEN12333 is a potent, selective and orally active α7 nAChR agonist. SEN12333 has a high affinity for rat α7 nAChRs expressed in GH4C1 cells (Ki=260 nM) and acts as a full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 was used in attention deficit disorder and schizophrenia studies. In whole-cell patch-clamp recordings, SEN12333 activated peak currents and maximum total charge similar to acetylcholine (EC50= 12 μM). SEN12333 has functional antagonistic effects on histamine H3 receptor (IC50=103 nM), and on the human ganglionic α3 nAChRs with weak agonistic activity (IC50= 8.5 μM)[1].

SEN12333 动物研究

Animal study Administered intraperitoneally at a dose of 3 mg/kg, SEN12333 improves episodic memory in rats during spontaneous amnesia as well as during a novel object recognition task in the presence of cognitive disturbances induced by glutamatergic or cholinergic mechanisms. SEN12333 also prevents memory deficits in a scopolamine-induced passive avoidance task[1].

SEN12333 参考文献

[1]Corinne Beinat, et al. The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases.Curr Pharm Des. 2016;22(14):2134-51.

SEN12333 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.73mL

2.95mL

1.47mL

29.46mL

5.89mL

2.95mL

SEN12333 技术信息

CAS号874450-44-9
分子式C20H25N3O2
分子量 339.431
别名 WAY-317538
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(309.34 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
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