Linopirdine dihydrochloride

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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)
Datasheet
Citations (12)
Reviews (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Product Action

View all Voltage-gated Potassium (KV) Channel Blockers

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

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

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

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


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.

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