Home Metabolism FAAH inhibitor JNJ-1661010 For research use only.

JNJ-1661010

Synonyms: Takeda-25

JNJ-1661010 (Takeda-25) is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.

JNJ-1661010 Chemical Structure

JNJ-1661010 Chemical Structure

CAS No. 681136-29-8

Purity & Quality Control

JNJ-1661010 Related Products

Signaling Pathway

FAAH Signaling Pathways

FAAH Signaling Pathway

Biological Activity

Description JNJ-1661010 (Takeda-25) is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.
Targets
FAAH (rat) [1] FAAH (human) [1]
10 nM 12 nM
In vitro
In vitro FAAH preincubated with JNJ-1661010 suggests a slow reversibility of the interaction between the JNJ-1661010 and the active site, which is accelerated at higher temperatures. [1] JNJ-1661010 is a covalent, mechanism-based substrate inhibitor as examined by LC-ESI-MS. JNJ-1661010 docks with the phenylthiadiazole in the hydrophobic tunnel and the phenylurea in the hydrophilic pocket of FAAH. [2]
In Vivo
In vivo JNJ-1661010 (20 mg/kg i.p.) inhibits FAAH by at least 85% for up to 4 h after dosing, resulting accumulation of lipid ethanolamides in rat brain. JNJ-1661010 dose-dependently reverses the tactile allodynia with a maximum efficacy of approximately 90% at 30 min postdose in both Mild Thermal Injury (MTI) mice and rat model. JNJ-1661010 (20 mg/kg) reverses tactile allodynia by 60.8% at 30 min in rat spinal nerve ligation injury model. JNJ-1661010 (50 mg/kg i.p.) shows a significant attenuation of the hyperalgesia at 30 min postdose in rat carrageenan model of inflammatory pain. [1] Rats dosed with JNJ-1661010 (20 mg/kg i.p.) has a plasma Cmax of 26.9 μM at the Tmax of 0.75 h and a Cmax in the brain of 6.04 μM at the Tmax of 2 h. JNJ-1661010 (20 mg/kg i.p.) inhibits brain FAAH and elevates AEA level in brain tissue in rat. [2]
Animal Research Animal Models Mild Thermal Injury (MTI) mice and rat models
Dosages 50 mg/kg
Administration Intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 365.45 Formula

C19H19N5OS
CAS No. 681136-29-8 SDF Download JNJ-1661010 SDF
Smiles C1CN(CCN1C2=NC(=NS2)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 36 mg/mL ( (98.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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