Cat. No.: HY-121422

JZP-361

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JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC₅₀ of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.63%
CAS No.: 1680193-80-9
Formule: C₂₂H₂₀ClN₅O
Masse moléculaire:405.88

Stockage:

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

JZP-361 Chemical Structure

CAS No.: 1680193-80-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

hMAGL

46 nM (IC₅₀)

hABHD6

1.79 μM (IC₅₀)

hFAAH

7.24 μM (IC₅₀)

H₁ Receptor

6.81 (pA2)

Voir tous les produits spécifiques à Isoform Histamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	7.24 μM Compound: JZP-361	Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting	[PMID: 26344596]
HEK293	IC₅₀	0.046 μM Compound: JZP-361	Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method	[PMID: 26344596]
HEK293	IC₅₀	1.78 μM Compound: JZP-361	Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method	[PMID: 26344596]
HEK293	IC₅₀	1.78 μM Compound: 12a, JZP-361	Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells Inhibition of human ABHD6 containing pCMV6-AC-hABHD6 transfected into HEK293 cells	[PMID: 25752982]

In Vitro

JZP-361 has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC₅₀ = 7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC₅₀ = 1.79 μM)^[1].
JZP-361 retains H₁ antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM^[1].
JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole^[1].

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

Chemical Information

CAS No. 1680193-80-9
Appearance Solid
Masse moléculaire 405.88
Formule C₂₂H₂₀ClN₅O
Color White to off-white
SMILES

O=C(N(CC/1)CCC1=C2C3=C(CCC4=C/2N=CC=C4)C=C(C=C3)Cl)N5N=CN=C5
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (307.97 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)

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

2.4638 mL

12.3189 mL

24.6378 mL

5 mM

0.4928 mL

2.4638 mL

4.9276 mL

10 mM

0.2464 mL

1.2319 mL

2.4638 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Jayendra Z Patel, et al. Loratadine analogues as MAGL inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1436-42. [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, 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	2.4638 mL	12.3189 mL	24.6378 mL	61.5946 mL
	5 mM	0.4928 mL	2.4638 mL	4.9276 mL	12.3189 mL
	10 mM	0.2464 mL	1.2319 mL	2.4638 mL	6.1595 mL
	15 mM	0.1643 mL	0.8213 mL	1.6425 mL	4.1063 mL
	20 mM	0.1232 mL	0.6159 mL	1.2319 mL	3.0797 mL
	25 mM	0.0986 mL	0.4928 mL	0.9855 mL	2.4638 mL
	30 mM	0.0821 mL	0.4106 mL	0.8213 mL	2.0532 mL
	40 mM	0.0616 mL	0.3080 mL	0.6159 mL	1.5399 mL
	50 mM	0.0493 mL	0.2464 mL	0.4928 mL	1.2319 mL
	60 mM	0.0411 mL	0.2053 mL	0.4106 mL	1.0266 mL
	80 mM	0.0308 mL	0.1540 mL	0.3080 mL	0.7699 mL
	100 mM	0.0246 mL	0.1232 mL	0.2464 mL	0.6159 mL

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JZP-361

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Histamine Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

JZP-361

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Histamine Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

JZP-361 Related Classifications

HY-121422 Related Classifications