MAGL-IN-1

COA

级别和纯度:

≥99%

CAS编号: 2324160-91-8
分子式: C₂₂H₂₄FNO₃
分子量: 369.43
PubChem编号: 138319671

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货号 (SKU)	包装规格	是否现货
M651730-5mg	5mg	期货
M651730-10mg	10mg	期货
M651730-25mg	25mg	期货
M651730-50mg	50mg	期货
M651730-100mg	100mg	期货

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MAGL (32) Metabolic Enzyme/Protease (4889) 脂质代谢 (4331)

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基本描述

规格或纯度	≥99%
英文名称	MAGL-IN-1
生化机理	MAGL-IN-1 是一种强效、选择性、可逆和竞争性的 MAGL 抑制剂，其 IC 50 为 80 nM。MAGL-IN-1 对人类乳腺癌、结直肠癌和卵巢癌细胞具有抗增殖作用。MAGL-IN-1 可阻断细胞内的 MAGL，也可阻断细胞外的 MAGL。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL , with an IC 50 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 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 IC 50 s 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 [ 3 H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC 50 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 IC 50 of 2.1 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 IC 50 s of 7.9, 21, 25, 57, and 15 μM, respectively. Was inactive against MRC5 (IC 50 >100 μM). 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 80 nM (MAGL)
纯度	≥99%

关联靶点（人）

MGLL Tchem 单甘油酯脂肪酶(Monoglyceride lipase) (4 活性数据)

点击查看靶蛋白信息： MGLL

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)

点击查看靶蛋白信息： CNR1

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CNR2 Tchem Cannabinoid CB2 receptor (16942 活性数据)

点击查看靶蛋白信息： CNR2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

MRC5 (9203 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

OVCAR-3 (48710 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

SK-OV-3 (52876 活性数据)

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活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Caov-3 cell line (328 活性数据)

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活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

HCT-116 (91556 活性数据)

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活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

MDA-MB-231 (73002 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

MGLL Tchem Monoglyceride lipase (1909 活性数据)

点击查看靶蛋白信息： MGLL

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

ABHD12 Tchem Monoacylglycerol lipase ABHD12 (195 活性数据)

点击查看靶蛋白信息： ABHD12

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Faah Anandamide amidohydrolase (3907 活性数据)

点击查看靶蛋白信息： Faah

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Abhd6 Monoacylglycerol lipase ABHD6 (221 活性数据)

点击查看靶蛋白信息： Abhd6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	未知
IIUPAC Name	[1-(2-fluoro-5-hydroxybenzoyl)piperidin-4-yl]-(4-propan-2-ylphenyl)methanone
INCHI	1S/C22H24FNO3/c1-14(2)15-3-5-16(6-4-15)21(26)17-9-11-24(12-10-17)22(27)19-13-18(25)7-8-20(19)23/h3-8,13-14,17,25H,9-12H2,1-2H3
InChi Key	WUUBZNFATQKRPH-UHFFFAOYSA-N
Smiles	CC(C)C1=CC=C(C=C1)C(=O)C2CCN(CC2)C(=O)C3=C(C=CC(=C3)O)F
Isomeric SMILES	CC(C)C1=CC=C(C=C1)C(=O)C2CCN(CC2)C(=O)C3=C(C=CC(=C3)O)F
PubChem CID	138319671
分子量	369.43

化学和物理性质

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

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