Art. -Nr.: HY-19559

JNJ-46778212

Name: JNJ-46778212
Brand: MedChemExpress
SKU: HY-19559
Price: 70.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: VU 0409551)

Kundenbewertung

Based on 1 Customer Validation

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC₅₀ of 260 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.58%
CAS. Nr.: 1363281-27-9
Formel: C₂₀H₁₇FN₂O₃
Molecular Weight:352.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JNJ-46778212 Chemical Structure

CAS. Nr.: 1363281-27-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC₅₀ of 260 nM.

IC₅₀ & Target

^[1]

mGlu5 Receptor

260 nM (EC₅₀)

Alle mGluR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	235 nM Compound: 162; VU0409551	Positive allosteric modulation of rat mGlu5 receptor expressed in HEK293 cells assessed as increase in calcium mobilization Positive allosteric modulation of rat mGlu5 receptor expressed in HEK293 cells assessed as increase in calcium mobilization	[PMID: 29939744]

In Vivo

In oral brain/plasma studies, JNJ-46778212 displays excellent CNS penetration^[1]. JNJ-46778212 enhances NMDAR function and rescues long-term potentiation in hippocampal slices obtained from SR^−/− mice. The administration of JNJ-46778212 to SR^−/− mice reverses their deficits in several neuroplasticity signaling pathways and improves their contextual fear memory^[2].

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

Chemical Information

CAS. Nr. 1363281-27-9
Appearance Solid
Molecular Weight 352.36
Formel C₂₀H₁₇FN₂O₃
Color Light yellow to yellow
SMILES

O=C(N1CCC2=C(OC(COC3=CC=CC=C3)=N2)C1)C4=CC=C(F)C=C4
Synonyms

VU 0409551
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (283.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8380 mL

14.1900 mL

28.3801 mL

5 mM

0.5676 mL

2.8380 mL

5.6760 mL

10 mM

0.2838 mL

1.4190 mL

2.8380 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Conde-Ceide S, et al. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015 May 20;6(6):716-20. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8380 mL	14.1900 mL	28.3801 mL	70.9502 mL
	5 mM	0.5676 mL	2.8380 mL	5.6760 mL	14.1900 mL
	10 mM	0.2838 mL	1.4190 mL	2.8380 mL	7.0950 mL
	15 mM	0.1892 mL	0.9460 mL	1.8920 mL	4.7300 mL
	20 mM	0.1419 mL	0.7095 mL	1.4190 mL	3.5475 mL
	25 mM	0.1135 mL	0.5676 mL	1.1352 mL	2.8380 mL
	30 mM	0.0946 mL	0.4730 mL	0.9460 mL	2.3650 mL
	40 mM	0.0710 mL	0.3548 mL	0.7095 mL	1.7738 mL
	50 mM	0.0568 mL	0.2838 mL	0.5676 mL	1.4190 mL
	60 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1825 mL
	80 mM	0.0355 mL	0.1774 mL	0.3548 mL	0.8869 mL
	100 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7095 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

JNJ-46778212

Alle mGluR Isoform-spezifische Produkte anzeigen