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JNJ-1661010

Name: JNJ-1661010
Brand: Selleck Chemicals
SKU: S2828

Catalog No.S2828 Synonyms: Takeda-25

For research use only.

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.

CAS No. 681136-29-8

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FAAH Signaling Pathway Map

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

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

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]

Protocol (from reference)

Animal Research:^[1]	Animal Models: Mild Thermal Injury (MTI) mice and rat models Dosages: 50 mg/kg Administration: Intraperitoneal injection

References

Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+95% Corn oil For best results, use promptly after mixing. Click to purchase: Corn Oil	5 mg/mL

Chemical Information

Molecular Weight	365.45
Formula	C₁₉H₁₉N₅OS
CAS No.	681136-29-8
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CN(CCN1C2=NC(=NS2)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4

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

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