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Terfenadine

Cat. No. 3948 5 篇引用文献 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）
Pricing Availability   Qty
说明： H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker
化学名： α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
纯度： ≥98% (HPLC)
说明书
引用文献 (5)
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 Terfenadine

Terfenadine is a histamine H1 receptor antagonist. Also blocks KV11.1 (hERG) and Kir6 (KATP) channels (IC50 values are 204 nM and 1.2 μM respectively). Inhibits the delayed rectifier K+ current (IKr) in guinea pig ventricular myocytes (IC50 = 50 nM). Activity prolongs QT and induces Torsades de pointes (TdP); cardiotoxic in vivo.

化合物库 for Terfenadine

Terfenadine is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for Terfenadine

分子量 471.67
公式 C32H41NO2
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 50679-08-8
PubChem ID 5405
InChI Key GUGOEEXESWIERI-UHFFFAOYSA-N
Smiles OC(C3=CC=CC=C3)(C4=CC=CC=C4)C1CCN(CCCC(O)C2=CC=C(C(C)(C)C)C=C2)CC1

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 Terfenadine

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 47.17 100
ethanol 11.79 25

制备储备液 for Terfenadine

以下数据基于产品分子量 471.67。 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 2.12 mL 10.6 mL 21.2 mL
5 mM 0.42 mL 2.12 mL 4.24 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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参考文献 for Terfenadine

参考文献是支持产品生物活性的出版物。

Crumb (2000) Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions. J.Pharmacol.Exp.Ther. 292 261 PMID: 10604956

Zunkler et al (2000) Mechanism of terfenadine block of ATP-sensitive K+ channels. Br.J.Pharmacol. 130 1571 PMID: 10928959

Stork et al (2007) State dependent dissociation of HERG channel inhibitors. Br.J.Pharmacol. 151 136 PMID: 17592502

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

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关键词: Terfenadine, Terfenadine supplier, hERG, Human, Ether-A-Go-Go, Gene, KV11.1, KIR6, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Potassium, KV, KATP, Channels, voltage-gated, voltage-dependent, Receptors, a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, Voltage-Gated, Histamine, Inward, rectifier, 3948, Tocris Bioscience

5 篇 Terfenadine 的引用文献

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

Pérez-Gómez et al (2018) A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia. Nat Commun 9 5272 PMID: 30532051

Masafumi et al (2021) Cardioluminescence in Transgenic Zebrafish Larvae: A Calcium Imaging Tool to Study Drug Effects and Pathological Modeling. Biomedicines 9 PMID: 34680411

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

Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469

Rui et al (2020) Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2. Mol Cancer Ther 19 2023-2033 PMID: 32855270

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Terfenadine 的评论

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Terfenadine was used to assess its action on BK channels.
By Anonymous on 12/03/2018
分析类型： In Vitro
种属： Human

Terfenadine was used to assess its action on BK channels, which are Calcium activated voltage-gated potassium channels that conduct large amounts of potassium ions (K+) across the cell membrane. Results were reliable and reproducible.

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Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.