JZL 184 是一种有效的,选择性的且不可逆的MAGL抑制剂,可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。JZL 184 对MAGL的选择性比 FAAH 高 300 倍以上。
生物活性 | JZL 184 is a potent, selective and irreversibleMAGLinhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50of 8 nM). JZL 184 displays >300-fold selectivity forMAGLoverFAAH[1][2]. |
IC50& Target | IC50: 8 nM (2-Arachidonoylglycerol (2-AG) hydrolysis)[1] |
体外研究 (In Vitro) | JZL 184 displays IC50values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells[1].
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体内研究 (In Vivo) | JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia[1]. JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons[2].
Animal Model: | Male C57Bl/6 mice (6-8 weeks old, 20-26 g)[1] | Dosage: | 4 mg/kg, 8 mg/kg, 16 mg/kg, 40 mg/kg | Administration: | Intraperitoneal injection; once | Result: | Produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that were maintained for at least 8 h. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 35 mg/mL(67.24 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.9213 mL | 9.6063 mL | 19.2127 mL | 5 mM | 0.3843 mL | 1.9213 mL | 3.8425 mL | 10 mM | 0.1921 mL | 0.9606 mL | 1.9213 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.80 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.80 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.80 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.80 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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