3-(环已氧羰基胺基)联苯
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- CAS号:
- 565460-15-3
- 英文名:
- URB602
- 英文别名:
- URB602;URB 602;URB-602;N-[1,1'-Biphenyl]-3-yl-;cyclohexyl biphenyl-3-ylcarbaMate;cyclohexyl N-(3-phenylphenyl)carbamate;Cyclohexyl [1,1'-biphenyl]-3-ylcarbaMate;Monoacylglycerol Lipase Inhibitor, URB602;Biphenyl-3-yl Carbamic Acid, Cyclohexyl Ester;[1,1’-Biphenyl]-3-yl-carbamic acid cyclohexyl ester;N-[1,1'-Biphenyl]-3-yl-carbamic acid cyclohexyl ester
- 中文名:
- 3-(环已氧羰基胺基)联苯
- 中文别名:
- 化合物URB602;3-(环已氧羰基胺基)联苯;URB602,MGL的抑制剂;MGL抑制剂(URB602);[1,1'-联苯]-3-基氨基甲酸环己酯
- CBNumber:
- CB4311681
- 分子式:
- C19H21NO2
- 分子量:
- 295.38
- MOL File:
- 565460-15-3.mol
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3-(环已氧羰基胺基)联苯化学性质
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熔点:
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122-123°C
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储存条件:
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2-8°C
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溶解度:
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DMSO: >10mg/mL
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形态:
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powder
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颜色:
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white to off-white
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3-(环已氧羰基胺基)联苯性质、用途与生产工艺
URB602是单酰基甘油脂酶(MGL)抑制剂。
IC50: 28±4 μM (rat brain MGL)
Without URB602, the apparent Michaelis constant (K
m
) of MGL for 2-AG is 24±1.7 μM and the maximum velocity (V
max
) is 1814±51 nmol min per mg protein; with URB602, the K
m
is 20±0.4 μM and the V
max
is 541±20 nmol min per mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca
2+
-ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased. URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). URB602 weakly inhibits recombinant MGL (IC
50
=223±63 μM) through a rapid and noncompetitive mechanism.
URB602 at doses of 20 and 40 mg/kg tends to reduce upper GI transit and slow colonic propulsion. When taken together as whole gut transit, URB602 dose dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of 40 mg/kg URB602 on whole gut transit is absent in these mice, indicating CB
1
receptor involvement in the inhibitory action. URB602 decreases the AUC of pain behaviour during the early phase of the formalin test with an ED
50
of 0.06±0.028 μg for JZL184 and 120±51.3 μg for URB602 in adult male Sprague-Dawley rats. Both MGL inhibitors also suppresses pain behaviour during the late phase of formalin pain, with an ED
50
of 0.03±0.011 μg for JZL184 and 66±23.9 μg for URB602.
用途
URB602 is a selective inhibitor of MGL, exhibiting an IC50 of 28 μM for the rat brain enzyme. It does not inhibit fatty acid amide hydrolase (FAAH) at concentrations up to 100 μM, or other lipid metab
olizing enzymes such as diacylglycerol lipase or cyclooxygenase-2.5 6 Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain a
nd stress management.
3-(环已氧羰基胺基)联苯
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-100792 | URB602 | | 5 mg | 300元 |
| 2024/01/25 | HY-100792 | 3-(环已氧羰基胺基)联苯
URB602 | 565460-15-3 | 10mM * 1mLin DMSO | 330元 |
565460-15-3, 3-(环已氧羰基胺基)联苯 相关搜索:
- Aromatics
- Pharmaceutical intermediate
- Inhibitors
- All Inhibitors
- Research Chemical
- Chemical for Research
- 药靶配体
- 细胞生物学试剂
- 合成
- URB602,MGL的抑制剂
- 化合物URB602
- MGL抑制剂(URB602)
- 3-(环已氧羰基胺基)联苯
- [1,1'-联苯]-3-基氨基甲酸环己酯
- 565460-15-3
- URB 602;URB-602
- N-[1,1'-Biphenyl]-3-yl-carbamic acid cyclohexyl ester
- cyclohexyl N-(3-phenylphenyl)carbamate
- Carbamic acid, N-[1,1'-biphenyl]-3-yl-, cyclohexyl ester
- Cyclohexyl [1,1'-biphenyl]-3-ylcarbaMate
- N-[1,1'-Biphenyl]-3-yl-
- Monoacylglycerol Lipase Inhibitor, URB602
- [1,1’-Biphenyl]-3-yl-carbamic acid cyclohexyl ester
- cyclohexyl biphenyl-3-ylcarbaMate
- Biphenyl-3-yl Carbamic Acid, Cyclohexyl Ester
- URB602