2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Licostinel

Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity.

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Licostinel

Licostinel Chemische Struktur

CAS. Nr. : 153504-81-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Beschreibung

Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity[1][2][3].

IC50 & Target

59 nM (glycine receptor)[1]
In Vivo
Animal Model: The permanent model of middle cerebral artery occlusion in fisher 344 rats and CD-1 mice.
The transient model of focal ischemia in Wistar and Sprague –Dawley rats [2
Dosage: 5 mg/kg bolus 3.5 mg/kg/h for 6h, 10 mg/kg bolus 7.0 mg/kg/h for 6h
Administration: A single intravenous injection bolus continuous infusion
Result: Decreased infarct size.
Animal Model: Male Sprague-Dawley rats [3]
Dosage: 20, 40, 80 mg/kg for intraperitoneal injection (i.p.) bolus 7 mg/kg/h , 30mins
Administration: Intravenous injection (i.v.) bolus continuous infusion
Result: Reduced the rate of spreading depression and EEG activity in the rat brain in a dose-dependent manner.
Molekulargewicht

276.04

Formel

C8H3Cl2N3O4
CAS. Nr.
Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C1NC2=C(NC1=O)C([N+]([O-])=O)=C(C(Cl)=C2)Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 12.5 mg/mL (45.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6227 mL 18.1136 mL 36.2273 mL
5 mM 0.7245 mL 3.6227 mL 7.2455 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6227 mL 18.1136 mL 36.2273 mL 90.5682 mL
5 mM 0.7245 mL 3.6227 mL 7.2455 mL 18.1136 mL
10 mM 0.3623 mL 1.8114 mL 3.6227 mL 9.0568 mL
15 mM 0.2415 mL 1.2076 mL 2.4152 mL 6.0379 mL
20 mM 0.1811 mL 0.9057 mL 1.8114 mL 4.5284 mL
25 mM 0.1449 mL 0.7245 mL 1.4491 mL 3.6227 mL
30 mM 0.1208 mL 0.6038 mL 1.2076 mL 3.0189 mL
40 mM 0.0906 mL 0.4528 mL 0.9057 mL 2.2642 mL
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Licostinel Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Licostinel153504-81-5ACEA-1021ACEA1021ACEA 1021iGluRIonotropic glutamate receptorsneuroprotectivestrokeGlyR antagonistInhibitorinhibitorinhibit

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