MAGL-IN-1 是一种有效,选择性,可逆和竞争性的MAGL抑制剂,IC50值为 80 nM。MAGL-IN-1 对人乳腺癌,结肠直肠癌和卵巢癌细胞具有抗增殖作用。MAGL-IN-1 在体内和体外均可阻断 MAGL。
生物活性 | MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor ofMAGL, with anIC50of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovariancancercells. MAGL-IN-1 blocksMAGLin cell-based as well as in vivo assays[1]. |
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体外研究 (In Vitro) | MAGL-IN-1 (compound 23) (0.02-200 μM; 96 h) produces an appreciable inhibition of cell viability in all the tested cancer cell lines, with IC50s ranging from 7.9 to 57 μM[1]. MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a Kiof 39 nM[1]. MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM[1]. MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [3H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC50of 193 nM[1]. MAGL-IN-1 (0.01-30 μM; 15 min) inhibits 2-OG hydrolysis in a concentration-dependent manner in mouse brain membrane preparations, with an IC50of 2.1 μM[1].
Cell Proliferation Assay[1] Cell Line: | HCT116, MDA-MB-231, CAOV3, OVCAR3, SKOV3, and MRC5 cells | Concentration: | 0.02-200 μM | Incubation Time: | 96 hours | Result: | Inhibited the growth of human breast MDA-MB-231, colorectal HCT116, and ovarian CAOV3, OVCAR3, and SKOV3 cancer cells, with IC50s of 7.9, 21, 25, 57, and 15 μM, respectively. Was inactive against MRC5 (IC50>100 μM). |
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体内研究 (In Vivo) | MAGL (compound 23) (50 mg/kg; a single i.p.) increases the 2-AG level in plasma and brain, and does not alter anandamide (AEA), arachidonic acid and prostaglandin levels in plasma and brain of mice[1].
Animal Model: | Male C57BL6 mice, 8-10 weeks old[1] | Dosage: | 50 mg/kg | Administration: | Intraperitoneal injection; once | Result: | Increased 2-AG levels in the brain and plasma. |
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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 : 62.5 mg/mL(169.18 mM;Need ultrasonic) 配制储备液 1 mM | 2.7069 mL | 13.5344 mL | 27.0687 mL | 5 mM | 0.5414 mL | 2.7069 mL | 5.4137 mL | 10 mM | 0.2707 mL | 1.3534 mL | 2.7069 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: 2.08 mg/mL (5.63 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.63 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 20.8 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: ≥ 2.08 mg/mL (5.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.63 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.63 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 20.8 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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