JNJ 1661010
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- CAS号:
- 681136-29-8
- 英文名:
- JNJ 1661010
- 英文别名:
- 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-;CS-1527;Takeda-25;JNJ 1661010;JNJ 1661010, >=98%;JNJ 1661010 USP/EP/BP;TAKEDA-25;JNJ-1661010;JNJ 1661010;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;broad-spectrum,acid,inhibit,hydrolase,barrier,JNJ-1661010,FAAH,Takeda25,Fatty acid amide hydrolase,amide,Takeda 25,blood-brain,Inhibitor,analgesics,Fatty
- 中文名:
- JNJ 1661010
- 中文别名:
- 化合物JNJ-1661010;JNJ-1661010游离态;JNJ-1661010,FAAH抑制剂;N-苯基-4-(3-苯基-1,2,4-噻二唑-5-基)哌嗪-1-酰胺;N-苯基-4-(3-苯基-1,2,4-噻二唑-5-基)-1-哌嗪甲酰胺
- CBNumber:
- CB92457306
- 分子式:
- C19H19N5OS
- 分子量:
- 365.45
- MOL File:
- 681136-29-8.mol
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JNJ 1661010化学性质
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密度:
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1.340±0.06 g/cm3(Predicted)
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储存条件:
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Sealed in dry,2-8°C
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溶解度:
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DMSO: ≥28mg/mL
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形态:
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solid
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酸度系数(pKa):
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13.94±0.70(Predicted)
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颜色:
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Off-white
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稳定性:
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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.
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JNJ 1661010性质、用途与生产工艺
JNJ-1661010是一种有效的，选择性的FAAH抑制剂，IC50分别为10 nM(大鼠)和12 nM (人类)，作用于FAAH-1比作用于FAAH-2选择性高100倍以上。
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.
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.
JNJ-1661010 (Takeda-25)是一种有效的，选择性的FAAH抑制剂，IC50分别为10 nM(大鼠)和12 nM (人类)，作用于FAAH-1比作用于FAAH-2选择性高100倍以上。
| Target | Value |
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FAAH (rat)
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10 nM
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FAAH (human)
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12 nM
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FAAH与JNJ-1661010预培养表明，JNJ-1661010和活性部位相互作用具有缓慢可逆性，并且在高温下会加速。 LC-ESI-MS检测表明，JNJ-1661010是一种共价的，基于机制的底物抑制剂。JNJ-1661010与苯基噻二唑在疏水性通道中对接，与苯脲在FAAH的亲水性口袋中对接。
JNJ-1661010(20 mg/kg i.p.)至少抑制85%的FAAH，给药后作用能维持4小时以上，导致大鼠大脑中脂质乙醇酰胺积累。温和热损伤的(MTI)小鼠和大鼠模型中，JNJ-1661010剂量依赖性逆转触觉异常疼痛，最大效能在给药30分钟后大约为90%。在大鼠脊髓神经结扎损伤模型中，JNJ-1661010 (20 mg/kg)给药30分钟时逆转60.8%触觉异常疼痛。在大鼠角叉菜胶炎性疼痛模型中，JNJ-1661010 (50 mg/kg i.p.)给药30分钟后显著减弱痛觉过敏。大鼠以JNJ-1661010 (20 mg/kg i.p.)给药，Tmax为0.75 h时，血浆Cmax为26.9 μM，Tmax为2 h时，大脑中Cmax为6.04 μM。JNJ-1661010 (20 mg/kg i.p.)抑制大鼠大脑中FAAH，并提高脑组织中AEA水平。
JNJ 1661010
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-N7062 | JNJ 1661010
JNJ-1661010 | 681136-29-8 | 5mg | 500元 |
| 2024/01/25 | HY-N7062 | JNJ 1661010
JNJ-1661010 | 681136-29-8 | 10mM * 1mLin DMSO | 550元 |
681136-29-8, JNJ 1661010 相关搜索:
- Inhibitor
- Inhibitors
- 合成有机化合物配体
- 抑制剂
- 代谢
- 小分子抑制剂，天然产物
- 小分子抑制剂
- JNJ-1661010,FAAH抑制剂
- N-苯基-4-(3-苯基-1,2,4-噻二唑-5-基)哌嗪-1-酰胺
- 化合物JNJ-1661010
- JNJ-1661010游离态
- N-苯基-4-(3-苯基-1,2,4-噻二唑-5-基)-1-哌嗪甲酰胺
- 681136-29-8
- broad-spectrum,acid,inhibit,hydrolase,barrier,JNJ-1661010,FAAH,Takeda25,Fatty acid amide hydrolase,amide,Takeda 25,blood-brain,Inhibitor,analgesics,Fatty
- 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-
- JNJ 1661010 USP/EP/BP
- TAKEDA-25;JNJ-1661010;JNJ 1661010
- N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
- CS-1527
- JNJ 1661010, >=98%
- Takeda-25
- N-Phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-1-piperazinecarboxamide
- JNJ 1661010