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Astemizole

Cat. No. 3489 1 次引用 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker
别名： Hismanal
化学名： 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
纯度： ≥99% (HPLC)
说明书
引用文献 (1)
评论 (1)
文献 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Astemizole

Astemizole is an orally active, potent histamine H1 antagonist (IC50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM). Also potent KV11.1 (hERG) channel blocker (IC50 = 0.9 nM) that displays cardiotoxicity in vivo.

技术数据 for Astemizole

分子量 458.57
公式 C28H31FN4O
储存 Store at +4°C
纯度 ≥99% (HPLC)
CAS Number 68844-77-9
PubChem ID 2247
InChI Key GXDALQBWZGODGZ-UHFFFAOYSA-N
Smiles FC(C=C5)=CC=C5CN2C1=CC=CC=C1N=C2NC3CCN(CCC4=CC=C(OC)C=C4)CC3

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Astemizole

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 45.86 100
ethanol 11.46 25

制备储备液 for Astemizole

以下数据基于产品分子量 458.57。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.18 mL 10.9 mL 21.81 mL
5 mM 0.44 mL 2.18 mL 4.36 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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产品说明书 for Astemizole

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Astemizole

参考文献是支持产品生物活性的出版物。

Cavalli et al (2002) Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers. J.Med.Chem. 45 3844 PMID: 12190308

Chong et al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415 PMID: 16816845

Laduron et al (1981) In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21 294 PMID: 6124876

If you know of a relevant reference for Astemizole, please let us know.

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关键词: Astemizole, Astemizole supplier, Potent, hERG, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Orally, active, potent, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Receptors, Histamine, KV11.1, Hismanal, Voltage-Gated, 3489, Tocris Bioscience

1 篇 Astemizole 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Astemizole 的部分引用包括：

Klingerman et al (2014) Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice. Schizophr Bull 40 327 PMID: 23328157

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Astemizole 的评论

平均评分: 5 (Based on 1 Review.)

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Astemizole was used to identify other potential Kv blockers.
By Anonymous on 10/31/2018
分析类型： In Vitro
种属： Human

Astemizole is a great well known histaminic drug which shows Kv channel blocking at high concentrations. It was used on our lab to identify other potential Kv blockers. While using it as a standard, it worked ideally all during the study period.

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Histamine Receptors Scientific Review

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