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681136-29-8

681136-29-8 structure
681136-29-8 structure
  • Name: JNJ-1661010
  • Chemical Name: N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
  • CAS Number: 681136-29-8
  • Molecular Formula: C19H19N5OS
  • Molecular Weight: 365.452
  • Catalog: Biochemical Inhibitor Metabolism FAAH inhibitor
  • Create Date: 2016-10-14 17:10:02
  • Modify Date: 2025-08-21 13:45:39
  • 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].

Name N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
Synonyms N1-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-
N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-1-piperazinecarboxamide
Description 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].
Related Catalog
Target

IC50: 34 nM (rat FAAH) and 33 nM (human FAAH)[1]

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].
References

[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.

Density 1.3±0.1 g/cm3
Melting Point 240.48 °C
Molecular Formula C19H19N5OS
Molecular Weight 365.452
Exact Mass 365.131042
PSA 89.60000
LogP 2.57
Index of Refraction 1.679
Storage condition Store at +4°C
Water Solubility DMSO: ≥28mg/mL

~82%

681136-29-8 structure

681136-29-8

Literature: Takeda Pharmaceutical Company Limited Patent: EP1813606 A1, 2007 ; Location in patent: Page/Page column 32-33 ;

~%

681136-29-8 structure

681136-29-8

Literature: Apodaca, Richard; Breitenbucher, J. Guy; Pattabiraman, Kanaka; Seierstad, Mark; Xiao, Wei Patent: US2007/4741 A1, 2007 ; Location in patent: Page/Page column 11; 14 ;
Precursor  3

DownStream  0

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