Linopirdine dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 1999 - Linopirdine dihydrochloride | C26H21N3O.2HCl | CAS No. 113168-57-3
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 (5)
Literature

Biological Activity

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

Linopirdine dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.44 100
ethanol 46.44 100
water 46.44 100

Preparing Stock Solutions

The following data is based on the product molecular weight 464.39. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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View Related Products by Product Action

View all Voltage-gated Potassium (KV) Channel Blockers

Keywords: Linopirdine dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, kv7, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, DuP996, DuP, 996, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience

5 Citations for Linopirdine dihydrochloride

Citations are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:

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

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

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

Ghezzi  et al (2016) Electrophysiological characterization of the M-current in rat hypoglossal motoneurons Neuroscience 340 62 PMID: 27984184


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