Art. -Nr.: HY-120727

VU0364289

Kundenbewertung

Based on 1 Customer Validation

VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC₅₀ of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.52%
CAS. Nr.: 1242443-29-3
Formel: C₂₀H₂₁N₃O₂
Molecular Weight:335.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

VU0364289 Chemical Structure

CAS. Nr.: 1242443-29-3

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

IC₅₀ & Target

mGlu₅

1.6 μM (EC₅₀)

Alle mGluR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	1.6 μM Compound: 10e, VU0364289	Positive allosteric modulation at rat mGluR5 receptor expressed in HEK293 cells assessed as glutamate-induced calcium fluorescence by Fluo-4/AM dye-based fluorescence assay Positive allosteric modulation at rat mGluR5 receptor expressed in HEK293 cells assessed as glutamate-induced calcium fluorescence by Fluo-4/AM dye-based fluorescence assay	[PMID: 23308336]

In Vivo

VU0364289 (10, 30, 56.6, 100 mg/kg ; i.p.; once) reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, and (56.6, 100 mg/kg) shows significantly fewer ambulations^[1].
VU0364289 (10 mg/kg; i.p.; once) is rapidly and significantly absorbed in rats, and shows excellent central nervous system penetration^[1].

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

Animal Model:

Adult male Sprague-Dawley rats (250-275 g)^[1].
Dosage:

10, 30, 56.6, 100 mg/kg
Administration:

Intraperitoneal injection; once.
Result:

Showed activity of reversing the hyperlocomotion induced by amphetamine, and can also significantly fewer ambulations in rats when dose up to 56.6 mg/kg.

Animal Model:

Adult male Sprague-Dawley rats (250-275 g)^[1].
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; once.
Result:

1.19 Pharmacokinetic Parameters of VU0364289 in male Sprague-Dawley rats^[1].

T_max (h) C_max (ng/mL) Plasma protein binding Rat Fu (free fraction)

IP (10 mg/kg) 0.25 1280 94% (h); 90% (r) 0.10

Chemical Information

CAS. Nr. 1242443-29-3
Appearance Solid
Molecular Weight 335.40
Formel C₂₀H₂₁N₃O₂
Color Yellow to brown
SMILES

N#CC1=CC=CC=C1N2CCN(CC2)C(COCC3=CC=CC=C3)=O
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 : 100 mg/mL (298.15 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

2.9815 mL

14.9076 mL

29.8151 mL

5 mM

0.5963 mL

2.9815 mL

5.9630 mL

10 mM

0.2982 mL

1.4908 mL

2.9815 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, 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

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: ≥ 2.5 mg/mL (7.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Gregory KJ, et al. N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. [Content Brief]

[2]. Ya Zhou, et al. Discovery of N-Aryl Piperazines as Selective mGluR5Potentiators with Improved In Vivo Utility. ACS medicinal chemistry letters, 2010, 1(8): 433-438.

[3]. Psychosis Models[M]//Melatonin, Neuroprotective Agents and Antidepressant Therapy. Springer, New Delhi, 2016: 731-750.

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, 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	2.9815 mL	14.9076 mL	29.8151 mL	74.5379 mL
	5 mM	0.5963 mL	2.9815 mL	5.9630 mL	14.9076 mL
	10 mM	0.2982 mL	1.4908 mL	2.9815 mL	7.4538 mL
	15 mM	0.1988 mL	0.9938 mL	1.9877 mL	4.9692 mL
	20 mM	0.1491 mL	0.7454 mL	1.4908 mL	3.7269 mL
	25 mM	0.1193 mL	0.5963 mL	1.1926 mL	2.9815 mL
	30 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4846 mL
	40 mM	0.0745 mL	0.3727 mL	0.7454 mL	1.8634 mL
	50 mM	0.0596 mL	0.2982 mL	0.5963 mL	1.4908 mL
	60 mM	0.0497 mL	0.2485 mL	0.4969 mL	1.2423 mL
	80 mM	0.0373 mL	0.1863 mL	0.3727 mL	0.9317 mL
	100 mM	0.0298 mL	0.1491 mL	0.2982 mL	0.7454 mL

Keywords

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

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

VU0364289

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle mGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

	T_max (h)	C_max (ng/mL)	Plasma protein binding	Rat Fu (free fraction)
IP (10 mg/kg)	0.25	1280	94% (h); 90% (r)	0.10

VU0364289

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle mGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

VU0364289 Related Classifications

HY-120727 Related Classifications