JZL 184|cas:1101854-58-3|西域试剂

JZL 184,98.06%

产品编号：Bellancom-15249| CAS NO：1101854-58-3| 分子式：C₂₇H₂₄N₂O₉| 分子量：520.49

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货号	价格	库存与货期
Bellancom-15249	￥515.00	杭州北京（现货）
Bellancom-15249	￥1700.00	杭州北京（现货）
Bellancom-15249	￥2890.00	杭州北京（现货）

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JZL 184

产品介绍

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 irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC₅₀ of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.

体外研究

JZL 184 displays IC₅₀ values 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57Bl/6 mice (6-8 weeks old, 20-26 g)
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57Bl/6 mice (6-8 weeks old, 20-26 g)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 35 mg/mL (67.24 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。