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Submit ReviewLinopirdine dihydrochloride
说明： KV7 (KCNQ) channel blocker
别名： DuP 996
化学名： 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
纯度： ≥99% (HPLC)
生物活性 for Linopirdine dihydrochloride
Linopirdine dihydrochloride is a blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
化合物库 for Linopirdine dihydrochloride
Linopirdine dihydrochloride 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 Linopirdine dihydrochloride
| 分子量 | 464.39 |
| 公式 | C26H21N3O.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 113168-57-3 |
| PubChem ID | 14209557 |
| InChI Key | ZEVVHCGTTNRYOY-UHFFFAOYSA-N |
| Smiles | Cl.Cl.O=C1N(C2=CC=CC=C2C1(CC1=CC=NC=C1)CC1=CC=NC=C1)C1=CC=CC=C1 |
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 Linopirdine dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 46.44 | 100 | |
| DMSO | 46.44 | 100 |
制备储备液 for Linopirdine dihydrochloride
以下数据基于产品分子量 464.39。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.77 mL | 21.53 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.31 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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产品说明书 for Linopirdine dihydrochloride
参考文献 for Linopirdine dihydrochloride
参考文献是支持产品生物活性的出版物。
Schnee and Brown (1998) Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J.Pharmacol.Exp.Ther. 286 709 PMID: 9694925
Wang et al (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 1890 PMID: 9836639
Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724 PMID: 9580619
If you know of a relevant reference for Linopirdine dihydrochloride, please let us know.
关键词: Linopirdine dihydrochloride, Linopirdine dihydrochloride supplier, KCNQ, channel, blockers, Potassium, KV, kv7, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, DuP996, DuP, 996, Voltage-Gated, 1999, Tocris Bioscience
12 篇 Linopirdine dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Linopirdine dihydrochloride 的部分引用包括：
Sedivy et al (2015) Role of Kv7 channels in responses of the pulmonary circulation to hypoxia. Am J Physiol Lung Cell Mol Physiol 308 L48 PMID: 25361569
Zampini et al (2013) Burst activity and ultrafast activation kinetics of CaV1.3 Ca2+ channels support presynaptic activity in adult gerbil hair cell ribbon synapses. Front Cell Neurosci 591 3811 PMID: 23713031
Joshi et al (2009) KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle. J Physiol 329 368 PMID: 19151245
Lecrux et al (2017) Impact of altered cholinergic tones on the neurovascular coupling response to whisker stimulation. J Neurosci 37 1518 PMID: 28069927
Luther and Birren (2009) p75 and TrkA signaling regulates sympathetic neuronal firing patterns via differential modulation of voltage-gated currents. J Neurosci 29 5411 PMID: 19403809
Anderson et al (2009) KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder. J.Urol 182 330 PMID: 19450820
Greene et al (2017) XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J.Pharmacol.Exp.Ther. 362 177 PMID: 28483800
Gigout et al (2012) Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex. BMC Neurosci 13 42 PMID: 22540185
Ghezzi et al (2016) Electrophysiological characterization of the M-current in rat hypoglossal motoneurons Neuroscience 340 62 PMID: 27984184
Zampini et al (2014) Fine Tuning of CaV1.3 Ca2+ channel properties in adult inner hair cells positioned in the most sensitive region of the Gerbil Cochlea. PLoS One 9 e113750 PMID: 25409445
Lee et al (2014) Serum starvation-induced voltage-gated potassium channel Kv7.5 expression and its regulation by Sp1 in canine osteosarcoma cells. Int J Mol Sci 15 977 PMID: 24434641
Carrott et al (2016) Absence of Neuroplastin-65 Affects Synaptogenesis in Mouse Inner Hair Cells and Causes Profound Hearing Loss. J Pharmacol Exp Ther 36 222 PMID: 26740663
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Linopirdine dihydrochloride 的评论
平均评分: 5 (Based on 1 Review.)
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Linopirdine proved to be a high quality Kv7 blocker and improves release of several neurotransmitters.
By
Sadequl Islam on 10/22/2018
分析类型： In Vitro
种属： Human
Our lab is working with Voltage gated potassium channel for a while and I have used a few potent Kv channel blockers to measure out the % blocking showed by them. This product gave reproducible data, stable in biological lab conditions and the work was published. So overall very happy with the purchase of the compound.
