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565460-15-3

中文名稱 3-(環(huán)已氧羰基胺基)聯(lián)苯
英文名稱 URB602
CAS 565460-15-3
分子式 C19H21NO2
分子量 295.38
MOL 文件 565460-15-3.mol
更新日期 2023/03/20 15:41:25
565460-15-3 結(jié)構(gòu)式 565460-15-3 結(jié)構(gòu)式

基本信息

中文別名
3-(環(huán)已氧羰基胺基)聯(lián)苯
[1,1'-聯(lián)苯]-3-基氨基甲酸環(huán)己酯
英文別名
URB602
N-[1,1'-Biphenyl]-3-yl-
URB602 ada@tuskwei.com whatsapp
cyclohexyl biphenyl-3-ylcarbaMate
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

物理化學(xué)性質(zhì)

熔點(diǎn)122-123°C
儲(chǔ)存條件2-8°C
溶解度二甲基亞砜:>10mg/mL
形態(tài)粉末
顏色白色至灰白色

應(yīng)用領(lǐng)域

用途1
URB602 is a selective inhibitor of MGL, exhibiting an IC50 of 28 碌M for the rat brain enzyme. It does not inhibit fatty acid amide hydrolase (FAAH) at concentrations up to 100 碌M, 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.

安全數(shù)據(jù)

WGK Germany3

常見(jiàn)問(wèn)題列表

生物活性
URB602是單?;视椭?MGL)抑制劑。
靶點(diǎn)

IC50: 28±4 μM (rat brain MGL)

體外研究

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.

體內(nèi)研究

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.

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