JNJ-1661010 - Moligand™, 10mM in DMSO , Inhibitor of Fatty acid amide hydrolase;Inhibitor of Fatty acid amide hydrolase-2, CAS No.681136-29-8, Inhibitor of Fatty acid amide hydrolase;Inhibitor of Fatty acid amide hydrolase-2

CAS: 681136-29-8 Cat. No.: J408111 Peso molecular: 365.45

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Takeda-25 | 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

JNJ-1661010 JNJ-1661010 (Takeda-25) 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.
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. 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.

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. 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.
Cell Data

cell lines：neonatal rat cardiomyocytes

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

Takeda-25 | 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1, 2, 4-thiadiazol-5-yl)-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

JNJ-1661010 (Takeda-25) 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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of Fatty acid amide hydrolase;Inhibitor of Fatty acid amide hydrolase-2

Nombres e identificadores

• Isómeros SMILES: C1CN(CCN1C2=NC(=NS2)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4
• Peso molecular: 365.45
• Reaxy-Rn: 12770748
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12770748&ln=

Objetivos asociados (humanos)

FAAH2 Tchem Fatty-acid amide hydrolase 2 (1 Activities)

Discover Target: FAAH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FAAH Tchem Fatty-acid amide hydrolase 1 (8 Activities)

Discover Target: FAAH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 240.48°C