MAGL-IN-1 - CAS:2324160-91-8

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MAGL-IN-1

目录号 : KM6530 CAS No. : 2324160-91-8 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC₅₀ of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.

体外研究

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.
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a K_i of 39 nM.
MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM.
MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC₅₀ of 193 nM.
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 IC₅₀ of 2.1 μM.

Cell Proliferation Assay

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).

体内研究

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.

Animal Model:	Male C57BL6 mice, 8-10 weeks old
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; once
Result:	Increased 2-AG levels in the brain and plasma.

分子式

C₂₂H₂₄FNO₃

分子量

369.43

CAS号

2324160-91-8

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

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (169.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°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: 2.08 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-CD in 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 μL 20% 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。