Art. -Nr.: HY-10864

URB-597

(Synonyms: KDS-4103)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC₅₀s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.

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Reinheit: 99.15%
CAS. Nr.: 546141-08-6
Formel: C₂₀H₂₂N₂O₃
Molecular Weight:338.40

Speicherung:

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

URB-597 Chemical Structure

CAS. Nr.: 546141-08-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	0.17 μM Compound: 1, URB597	Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate preincubated for 10 mins before substrate addition measured after 10 mins by liquid scintillation counting analysis Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate preincubated for 10 mins before substrate addition measured after 10 mins by liquid scintillation counting analysis	[PMID: 24083878]
HEK293	EC₅₀	0.1 μM Compound: URB597	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	[PMID: 30878828]
HEK293	EC₅₀	24.5 μM Compound: 50	Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx	[PMID: 20356305]
HEK293	IC₅₀	0.7 nM Compound: 3, URB-597	Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay	10.1039/C2MD00307D
HEK293	IC₅₀	11 nM Compound: 1a, URB-597	Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 60 mins before substrate addition by [3H]anandamide carbon filtration assay Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 60 mins before substrate addition by [3H]anandamide carbon filtration assay	[PMID: 19072118]
HEK293	IC₅₀	16 nM Compound: 1a, URB-597	Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 30 mins before substrate addition by [3H]anandamide carbon filtration assay Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 30 mins before substrate addition by [3H]anandamide carbon filtration assay	[PMID: 19072118]
HEK293	IC₅₀	2.3 nM Compound: 3, URB-597	Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay	10.1039/C2MD00307D
HEK293	IC₅₀	2187 nM Compound: 1a, URB-597	Inhibition of human recombinant FAAH expressed in HEK293 cells by [3H]anandamide carbon filtration assay Inhibition of human recombinant FAAH expressed in HEK293 cells by [3H]anandamide carbon filtration assay	[PMID: 19072118]
HEK293	IC₅₀	47 nM Compound: 1a, URB-597	Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 5 mins before substrate addition by [3H]anandamide carbon filtration assay Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 5 mins before substrate addition by [3H]anandamide carbon filtration assay	[PMID: 19072118]
Sf21	IC₅₀	0.26 μM Compound: URB597	Inhibition of human recombinant FAAH expressed in sf21 cells using AMC-AA as substrate preincubated for 15 mins followed by substrate addition measured after 2 hrs by spectrophotometric analysis Inhibition of human recombinant FAAH expressed in sf21 cells using AMC-AA as substrate preincubated for 15 mins followed by substrate addition measured after 2 hrs by spectrophotometric analysis	[PMID: 27117424]

In Vitro

URB-597 (KDS-4103) prevents the FAAH-catalyzed hydrolysis of [³H]anandamide by primary cultures of rat cortical neurons with an IC₅₀ value of ~0.50 nM^[1].

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

In Vivo

URB-597 (KDS-4103) inhibits rat brain FAAH activity after intraperitoneal (i.p.) administration with a median inhibitory dose (ID₅₀) of 0.15 mg/kg in wild-type mice (+/+) or FAAH-null mice (-/-)^[1].
KDS-4103 (0.1-0.3 mg/kg, i.p.) elicits significant, anxiolytic-like, antidepressant-like and analgesic effects, which are prevented by treatment with CB1 receptor antagonists in rats and mice^[1].
KDS-4103 is orally available in rats and cynomolgus monkeys^[1].
URB-597 inhibits FAAH in the brain rapidly (1 h), sustains at >90% through 12 h and >60% through 24 h after an oral dose of 10 mg/kg.

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

Animal Model:

Wistar rats^[1]
Dosage:

250, 500, 750, 1000, 1250 mg/kg (Pharmacokinetic Analysis)
Administration:

Oral administration
Result:

Absorbed at a moderate rate with peak plasma concentrations (C_max) achieved at 1.2 h after treatment. The oral elimination half-life was approximately 2 h.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 546141-08-6
Appearance Solid
Molecular Weight 338.40
Formel C₂₀H₂₂N₂O₃
Color White to off-white
SMILES

O=C(OC1=CC(C2=CC=CC(C(N)=O)=C2)=CC=C1)NC3CCCCC3
Synonyms

KDS-4103
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

Publications (5)

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Journal Impact Factor

Phytomedicine

Schisandra chinensis lignans regulate and cooperate with endogenous cannabinoid systems to ameliorate intestinal barrier injury associated with depression. [Abstract]

2024 Jul 31:133:155929. PMID: 39126923
J Neuroimmune Pharmacol

Alleviating CB2-Dependent ER Stress and Mitochondrial Dysfunction Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairment. [Abstract]

2024 Jan 12;19(1):1. PMID: 38214766
Eur J Pharmacol

URB597 exerts neuroprotective effects against transient brain ischemia injury in mice by regulating autophagic flux and necroptosis. [Abstract]

2023 Oct 15:957:175982. PMID: 37572942
Cereb Cortex

Activation of Oxytocin Receptors Excites Subicular Neurons by Multiple Signaling and Ionic Mechanisms. [Abstract]

2021 Mar 31;31(5):2402-2415. PMID: 33341872
Oxid Med Cell Longev

URB597 and Andrographolide Improve Brain Microvascular Endothelial Cell Permeability and Apoptosis by Reducing Oxidative Stress and Inflammation Associated with Activation of Nrf2 Signaling in Oxygen-Glucose Deprivation. [Abstract]

2022 May 12;2022:4139330. PMID: 35602108

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (295.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

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

2.9551 mL

14.7754 mL

29.5508 mL

5 mM

0.5910 mL

2.9551 mL

5.9102 mL

10 mM

0.2955 mL

1.4775 mL

2.9551 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: 10 mg/mL (29.55 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 10 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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 (7.39 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (273 KB)
SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 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]. Daniele Piomelli, et al. Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597). CNS Drug Rev. Spring 2006;12(1):21-38. [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	2.9551 mL	14.7754 mL	29.5508 mL	73.8770 mL
	5 mM	0.5910 mL	2.9551 mL	5.9102 mL	14.7754 mL
	10 mM	0.2955 mL	1.4775 mL	2.9551 mL	7.3877 mL
	15 mM	0.1970 mL	0.9850 mL	1.9701 mL	4.9251 mL
	20 mM	0.1478 mL	0.7388 mL	1.4775 mL	3.6939 mL
	25 mM	0.1182 mL	0.5910 mL	1.1820 mL	2.9551 mL
	30 mM	0.0985 mL	0.4925 mL	0.9850 mL	2.4626 mL
	40 mM	0.0739 mL	0.3694 mL	0.7388 mL	1.8469 mL
	50 mM	0.0591 mL	0.2955 mL	0.5910 mL	1.4775 mL
	60 mM	0.0493 mL	0.2463 mL	0.4925 mL	1.2313 mL
	80 mM	0.0369 mL	0.1847 mL	0.3694 mL	0.9235 mL
	100 mM	0.0296 mL	0.1478 mL	0.2955 mL	0.7388 mL

Keywords

URB-597

5 Cited Publications

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URB-597

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Publications Citing Use of MedChemExpress (MCE) URB-597

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

URB-597

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Mitochondria-Targeted Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Human Metabolite Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) URB-597

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

URB-597 Related Classifications

HY-10864 Related Classifications