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JNJ-1661010 FAAH inhibitor

Cat.No.S2828

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 FAAH inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 365.45

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Quality Control

Batch: Purity: 99.70%
99.70

Solubility

In vitro
Batch:

DMSO : 36 mg/mL (98.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 365.45 Formula

C19H19N5OS

 Storage (From the date of receipt)
CAS No. 681136-29-8 Download SDF Storage of Stock Solutions

Synonyms Takeda-25 Smiles C1CN(CCN1C2=NC(=NS2)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4

Mechanism of Action

Targets/IC50/Ki
FAAH (rat)
10 nM
FAAH (human)
12 nM
In vitro
FAAH preincubated with JNJ-1661010 suggests a slow reversibility of the interaction between this compound and the active site, which is accelerated at higher temperatures. This compound is a covalent, mechanism-based substrate inhibitor as examined by LC-ESI-MS. It docks with the phenylthiadiazole in the hydrophobic tunnel and the phenylurea in the hydrophilic pocket of FAAH.
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. This compound 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. It (20 mg/kg) reverses tactile allodynia by 60.8% at 30 min in rat spinal nerve ligation injury model. This chemical (50 mg/kg i.p.) shows a significant attenuation of the hyperalgesia at 30 min postdose in rat carrageenan model of inflammatory pain. Rats dosed with this compound (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. It (20 mg/kg i.p.) inhibits brain FAAH and elevates AEA level in brain tissue in rat.
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