JNJ-1661010

Catalog No.S2828

JNJ-1661010 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.

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JNJ-1661010 Chemical Structure

JNJ-1661010 Chemical Structure
Molecular Weight: 365.45

Validation & Quality Control

Quality Control & MSDS

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JNJ-1661010 is available in the following compound libraries:

Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description JNJ-1661010 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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

FAAH Preincubation Assay SK-N-MC cells expressing either human or rat recombinant FAAH are homogenized in FAAH assay buffer (125 mM Tris, 1 mM EDTA, 0.2% glycerol, 0.02% Triton X-100, 0.4 mM HEPES, pH 8 and diluted to a final protein concentration of 70 μg/mL. Unless otherwise indicated, the assay mixture consist of 80 μL of the cell homogenate, 10 μL of the appropriate inhibitor (JNJ-1661010), and 10 μL of 80 nM [3H]-AEA (final concentration). The reactions are performed at room temperature (22 °C). Before addition of substrate, assay mix is preincubated for 0 min, 10 min, 20 min, or 40 min. Enzymatic activity is assayed and measured as described previously. Under the conditions used, the assay is linear for at least 2 hours, and the enzyme typically hydrolyzes <10% of available substrate.

Animal Study: [1]

Animal Models Mild Thermal Injury (MTI) mice and rat models
Formulation 5% Pharmasolve: 20% Cremophor: 75% saline
Dosages 50 mg/kg
Administration Intraperitoneal injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Karbarz MJ, et al. Anesth Analg, 2009, 108(1), 316-329.

[2] Keith JM, et al. Bioorg Med Chem Lett, 2008, 18(17), 4838-4843.

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Chemical Information

Download JNJ-1661010 SDF
Molecular Weight (MW) 365.45
Formula

C19H19N5OS

CAS No. 681136-29-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Takeda-25
Solubility (25°C) * In vitro DMSO 36 mg/mL (98.5 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+95% Corn oil 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-

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.

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