Bioactivity | JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics[1][2]. | ||||||||||||
Target | IC50: 34 nM (rat FAAH) and 33 nM (human FAAH) | ||||||||||||
In Vivo | JNJ-1661010 (Takeda-25; i.p.; 50 mg/kg) diminishes thermal hyperalgesia in the inflammatory rat carrageenan paw model[2]. JNJ-1661010 (i.p.; 10 mg/kg) has a T1/2 of 35 mins, a CL of 0.032 mL/min/kg, and a Cmax of 1.58 μM for rats[1]. | ||||||||||||
Name | JNJ-1661010 | ||||||||||||
CAS | 681136-29-8 | ||||||||||||
Formula | C19H19N5OS | ||||||||||||
Molar Mass | 365.45 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Keith JM, et al. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. [2]. Karbarz MJ, et al. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylicacid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. |