681136-29-8
JNJ-1661010
CAS: 681136-29-8
Molecular Formula: C19H19N5OS
681136-29-8 - Names and Identifiers
681136-29-8 - Physico-chemical Properties
| Molecular Formula | C19H19N5OS |
| Molar Mass | 365.45 |
| Density | 1.340±0.06 g/cm3(Predicted) |
| Melting Point | 240.48℃ |
| Solubility | Soluble in DMSO (36 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ |
| Appearance | solid |
| Color | Off-white |
| pKa | 13.94±0.70(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| Use | A selective and reversible inhibitor of fatty acid amide hydrolase (FAAH). |
| In vitro study | Preincubation of FAAH with JNJ-1661010 showed that JNJ-1661010 and active site interactions were slowly reversible and accelerated at high temperatures. LC-ESI-MS assays indicate that JNJ-1661010 is a covalent, mechanism-based substrate inhibitor. JNJ-1661010 docked with phenythiadiazole in the hydrophobic channel and with phenylurea in the hydrophilic pocket of FAAH. |
| In vivo study | JNJ-1661010(20 mg/kg I. p.) inhibited FAAH by at least 85% and the effect was maintained for more than 4 h after administration, resulting in accumulation of lipid ethanolamide in the rat brain. In mild heat-injured (MTI) mouse and rat models, JNJ-1661010 dose-dependently reverses tactile allodynia, with maximal efficacy of approximately 90% at 30 minutes after administration. In a rat spinal nerve ligation injury model, JNJ-1661010 (20 mg/kg) reversed 60.8% tactile allodynia at 30 min. In the rat carrageenan inflammatory pain model, JNJ-1661010 (50 mg/kg I. p.) significantly attenuated hyperalgesia 30 minutes after administration. Rats were treated with JNJ-1661010 (20 mg/kg I. p.) administration, a plasma Cmax of 26.9 μm at Tmax of 0.75 h and a Cmax of 6.04 μm in the brain at Tmax of 2 h. JNJ-1661010 (20 mg/kg I. p.) inhibited FAAH in rat brain and increased AEA levels in brain tissue. |
681136-29-8 - Risk and Safety
| WGK Germany | 1 |
681136-29-8 - Introduction
JNJ-1661010 is an effective and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), respectively, which is more than 100 times more selective in FAAH-1 than in FAAH-2.
Last Update：2022-10-16 17:41:45
681136-29-8 - Reference Information
| biological activity | JNJ-1661010 is an effective and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), respectively, acting on FAAH-1 is more than 100 times more selective than acting on FAAH-2. JNJ-1661010 (Takeda-25) is an effective and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human) respectively, which is more than 100 times more selective in FAAH-1 than in FAAH-2. |
| Target | Value |
| FAAH (rat) | 10 nM |
| FAAH (human) | 12 nM |
Last Update：2024-04-09 20:49:11
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Product Name: JNJ-1661010 Visit Supplier Webpage Request for quotation
CAS: 681136-29-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 681136-29-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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