JNJ-1661010 |cas 681136-29-8 |From Supplier DC Chemicalsicals

JNJ-1661010 |cas 681136-29-8 |From Supplier DC Chemicalsicals 

DC Chemicals supplies: JNJ-1661010,cas: 681136-29-8,Catalog: DC7617,In stock.

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Product name: JNJ-1661010, Synonyms: Takeda-25,JNJ-1661010,JNJ 1661010, cas: 681136-29-8, MW: 365.45, Molecule Formula: C19H19N5OS

JNJ-1661010, cas: 681136-29-8, Purity:>98%,Supplied by DC ChemicalsJNJ-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.

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] 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]For the detailed information of JNJ-1661010, the solubility of JNJ-1661010 in water, the solubility of JNJ-1661010 in DMSO, the solubility of JNJ-1661010 in PBS buffer, the animal experiment (test) of  JNJ-1661010, the cell expriment (test) of JNJ-1661010, the in vivo, in vitro and clinical trial test of JNJ-1661010, the EC50, IC50,and Affinity of JNJ-1661010, Please contact DC Chemicals.