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ABT-239 {[allProObj[0].p_purity_real_show]}

货号：A663348

ABT-239 is a highly efficacious, non-imidazole class of H3R antagonist.

ABT-239 化学结构 CAS号：460746-46-7
ABT-239 化学结构
CAS号：460746-46-7
ABT-239 3D分子结构
CAS号：460746-46-7
ABT-239 化学结构 CAS号：460746-46-7
ABT-239 3D分子结构 CAS号：460746-46-7
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ABT-239 纯度/质量文件 产品仅供科研

货号：A663348 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 2HCl ✔ 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 ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
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。

ABT-239 生物活性

描述 Histaminergic H3 receptors (H3R) antagonists enhance cognition in preclinical models and modulate neurotransmission, in particular acetylcholine (ACh) release in the cortex and hippocampus, two brain areas involved in memory processing. ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist[3]. ABT-239 (10 μM) increased histamine release from the TMN (tuberomamillary nucleus), NBM (nucleus basalis magnocellularis), and cortex[4]. ABT-239 (3 mg/kg, i.p.) ameliorated the cognitive performance in the ORT (object recognition test). ABT-239 systemic treatments increased GSK-3β phosphorylation in cortical and hippocampal homogenates of normal mice[3]. ABT-239 (1 and 3 mg/kg; i.p.) significantly attenuated KA (Kainic acid)-mediated behavioural and excitotoxic anomalies and restored altered expression of Bax, cleaved caspase-3, phospho-Akt (Ser473) and cAMP response element binding protein (CREB)[5].

ABT-239 参考文献

[1]Provensi G, Costa A, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacology. 2016 Oct;109:139-147.

[2]Bhowmik M, Saini N, et al. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.

[3]Provensi G, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacology. 2016 Oct;109:139-147.

[4]Munari L, et al. Selective brain region activation by histamine H₃ receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40。

[5]Bhowmik M, et al. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.

ABT-239 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.13mL

3.03mL

1.51mL

30.26mL

6.05mL

3.03mL

ABT-239 技术信息

CAS号460746-46-7
分子式C22H22N2O
分子量 330.42
SMILES Code N#CC1=CC=C(C2=CC=C(OC(CCN3[C@H](C)CCC3)=C4)C4=C2)C=C1
MDL No. MFCD13248643
别名
运输蓝冰
InChI Key KFHYZKCRXNRKRC-MRXNPFEDSA-N
Pubchem ID 9818903
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 105 mg/mL(317.77 mM)，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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: ABT-239 | 460746-46-7 | ABT239 | ABT 239 | Histamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Membrane Transporter/Ion Channel | Histamine Receptor | TRP Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | ABT-239 纯度/质量文件 | ABT-239 亚型比较 | ABT-239 生物活性 | ABT-239 参考文献 | ABT-239 实验方案 | ABT-239 技术信息

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