1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Potassium Channel
    TRP Channel
  3. Linopirdine

Linopirdine (Synonyms: DuP 996)

Cat. No.: HY-W020468 Purity: 98.83%
Handling Instructions

Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.

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Linopirdine Chemical Structure

Linopirdine Chemical Structure

CAS No. : 105431-72-9

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10 mM * 1  mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
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Description

Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3].

IC50 & Target

IC50: 2.4 μM (M-type K+ current)[1]

In Vitro

Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K+ leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na+/K+ inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC50>300 μM)[1].
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1)[3].

In Vivo

Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%[2].

Animal Model: Male Sprague-Dawley rats (300-350 g)[2]
Dosage: 0.1, 0.5, 1, 3, 6 mg/kg
Administration: 5 intravenous bolus injections of increasing doses
Result: Transiently and dose-dependently increases MAP by up to 15%.
Molecular Weight

391.46

Formula

C₂₆H₂₁N₃O

CAS No.

105431-72-9

SMILES

O=C1N(C2=CC=CC=C2)C3=C(C=CC=C3)C1(CC4=CC=NC=C4)CC5=CC=NC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (319.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5545 mL 12.7727 mL 25.5454 mL
5 mM 0.5109 mL 2.5545 mL 5.1091 mL
10 mM 0.2555 mL 1.2773 mL 2.5545 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LinopirdineDuP 996DuP996DuP-996Potassium ChannelTRP ChannelKcsATransient receptor potential channelsorallyM-typeK+currentIMKv7KCNQChannelsTRPV1cognitionenhancingacetylcholineInhibitorinhibitorinhibit

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Linopirdine
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