Linopirdine dihydrochloride

Name: Linopirdine dihydrochloride
Brand: Tocris Bioscience
SKU: 1999
Rating: 5 (1 reviews)

Catalog # 1999 | Tocris Bioscience a Bio-Techne Brand

(1)

Citations (12)

COA / SDS

KV7 (KCNQ) channel blocker

Key Product Details

Description:	K_V7 (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)
Molecular Weight:	464.39

View Full Technical Details for Linopirdine dihydrochloride

Technical Data
Citations (12) / Reviews (1)

Biological Activity for Linopirdine dihydrochloride

Linopirdine dihydrochloride is a blocker of K_V7 (KCNQ) voltage-gated potassium channels; blocks K_V7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC₅₀ = 4 - 7 μM) and K_V7.1 (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 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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References for Linopirdine dihydrochloride

References are publications that support the biological activity of the product.

Schnee and Brown 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. 1998 PMID: 9694925
Wang KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998 PMID: 9836639
Zaczek 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. 1998 PMID: 9580619

Citations for Linopirdine dihydrochloride (12)

Showing 1 - 10 of 12 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for Linopirdine dihydrochloride include:

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
Lecrux et al. (2017) Impact of altered cholinergic tones on the neurovascular coupling response to whisker stimulation. J Neurosci. 37:1518
PMID: 28069927
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
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. (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
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
Gigout et al. (2012) Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex. BMC Neurosci. 13:42
PMID: 22540185
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
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
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

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Customer Reviews for Linopirdine dihydrochloride (1)

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Linopirdine proved to be a high quality Kv7 blocker and improves release of several neurotransmitters

Name: Sadequl Islam

Species: Human

Assay Type: In Vitro

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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