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Submit ReviewLinopirdine dihydrochloride
Description: KV7 (KCNQ) channel blocker
Alternative Names: DuP 996
Chemical Name: 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity 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.
Compound Libraries for Linopirdine dihydrochloride
Linopirdine dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Linopirdine dihydrochloride
| M. Wt | 464.39 |
| Formula | C26H21N3O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Linopirdine dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 46.44 | 100 | |
| DMSO | 46.44 | 100 |
Preparing Stock Solutions for Linopirdine dihydrochloride
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for Linopirdine dihydrochloride
References for Linopirdine dihydrochloride
References are publications that support the biological activity of the product.
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.
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Keywords: 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 Citations for Linopirdine dihydrochloride
Citations are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:
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
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
Lecrux et al (2017) Impact of altered cholinergic tones on the neurovascular coupling response to whisker stimulation. J Neurosci 37 1518 PMID: 28069927
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
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
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
Do you know of a great paper that uses Linopirdine dihydrochloride from Tocris? Please let us know.
Reviews for Linopirdine dihydrochloride
Average Rating: 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
Assay Type: In Vitro
Species: 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.
