JNJ-1661010
- Takeda-25
货号: abs813688
货号-规格 | 货期 | 价格 | 数量 |
abs813688-10mg | 1-2周 | ¥945.00 | - + |
abs813688-25mg | 1-2周 | ¥2091.00 | - + |
abs813688-50mg | 1-2周 | ¥3251.00 | - + |
abs813688-100mg | 1-2周 | ¥5204.00 | - + |

产品描述 | ||
描述 | JNJ-1661010 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. | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | Takeda-25 | |
外观 | 白色粉末 | |
可溶性/溶解性 | Ethanol :3.7 mg/mL (10 mM) DMSO :36.6 mg/mL (100 mM) | |
生物活性 | ||
靶点 | FAAH (rat),FAAH (human) | |
In vitro(体外研究) | 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(体内研究) | 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. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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