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TAK 21d

Names

[ CAS No. ]:
1143578-94-2

[ Name ]:
TAK 21d

[Synonym ]:
1-Piperazinecarboxamide, 4-[4-(3,4-difluorophenyl)-2-pyrimidinyl]-N-3-pyridazinyl-
4-[4-(3,4-Difluorophenyl)-2-pyrimidinyl]-N-(3-pyridazinyl)-1-piperazinecarboxamide

Biological Activity

[Description]:

FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> FAAH
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> FAAH

[Target]

IC50: 0.72 nM (hFAAH); 0.28 nM (rFAAH)[1]


[In Vivo]

FAAH-IN-6 (compound 21d) (1-10 mg/kg; p.o.) shows significantly ameliorates tactile allodynia in a dose-dependent fashion in SNI-induced neuropathic pain rats model[1]. FAAH-IN-6 (3-10 mg/kg; p.o.) shows significantly ameliorates tactile allodynia of the ipsilateral hind paw in CFA-induced inflammatory pain model[1].

[References]

[1]. Kono M, et al. Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors. Bioorg Med Chem. 2014 Feb 15;22(4):1468-78.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C19H17F2N7O

[ Molecular Weight ]:
397.381

[ Exact Mass ]:
397.146271

[ LogP ]:
1.43

[ Index of Refraction ]:
1.645

Related Compounds