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[CAS NO. 105431-72-9] Linopirdine
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-W020468 |
| Brand: | MCE |
| CAS: | 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 |
1 Publications Citing Use of MCE
Summary
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
DMSO : 125 mg/mL ( 319.32 mM ; Need ultrasonic)
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 |
References
- [1] Schnee ME, et al. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998 Aug;286(2):709-17.
- [2] Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8.
- [3] Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40.
Synonyms
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