[CAS NO. 105431-72-9] Linopirdine

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PRODUCTS SPECIFICATIONS [105431-72-9]

Catalog

HY-W020468

Brand

MCE

CAS

105431-72-9

DESCRIPTION [105431-72-9]

Overview

MDL	MFCD00867216
Molecular Weight	391.46
Molecular Formula	C26H21N3O
SMILES	O=C1N(C2=CC=CC=C2)C3=C(C=CC=C3)C1(CC4=CC=NC=C4)CC5=CC=NC=C5

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Curr Biol. 2022 Jul 13;S0960-9822(22)01079-X.

Summary

Linopirdine (DuP 996) is an orally active, selective M-type K ⁺ current (IM; Kv7; KCNQ Channels) inhibitor with an IC ₅₀ 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 IC ₅₀ 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 (IC ₅₀ >300 μM) ^[1] .
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1) ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

Appearance

Solid

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 available by MCE.

References

Synonyms

2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-

1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one

DuP 996

Linopirdine

1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one