吗氯贝胺, 单胺氧化酶 A 抑制剂

MAO-A 选择性抑制剂

Moligand™

10mM in DMSO

CAS编号: 71320-77-9(DMSO)
分子式: C₁₃H₁₇ClN₂O₂
分子量: 268.74

有货

库存信息

关闭

货号 (SKU)	包装规格	是否现货	价格	数量
M408871-1ml	1ml	现货

查看相关系列

Compound libraries (12332)

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

英文别名	4-Chloro-N-(2-morpholin-4-ylethyl)benzamide
规格或纯度	Moligand™, 10mM in DMSO
英文名称	Moclobemide (Ro 111163)
生化机理	莫氯贝胺是一种 MAO-A（5-羟色胺）抑制剂，IC50 为 6.1 μM。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	抑制剂
作用机制	单胺氧化酶 A 抑制剂
产品介绍	Moclobemide (Ro 111163)是一种MAO-A (5-HT)抑制剂，IC50为6.1 μM。A reversible monoamine oxidase inhibitor. Information Moclobemide is aMAO-A (5-HT)inhibitor withIC50of 6.1 μM. In vitro Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat brain with ED50 of 7.6 μmol/kg and 78 μmol/kg, respectively. Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. Moclobemide (0.1 mM), which inhibits brain MAO-A activity by over 80%, does not affect benzylamine oxidase (rat heart) and diamine oxidase (rat small intestine) activity in vitro. Moclobemide (10 mM-100 mM) includes in the culture medium during anoxia or with glutamate significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex. In vivo Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. Moclobemide, given via the drinking water (4.5 mg/kg/day), produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. Moclobemide upregulates hippocampal mineralocorticoid receptor (MR) levels in rats by 65%, 76% and 19% at 2 weeks, 5 weeks and 7 weeks of treatment, and upregulates Glucocorticoid receptor (GR) levels in this limbic brain structure by 10% at 5 weeks. Moclobemide treatment (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. Moclobemide (2.5 mg/kg/day) decreases immobility and increases climbing behavior following treatment for 3 days, but increases in both swimming and climbing behaviors are measured following treatment for 14 days. Moclobemide (15 mg/kg/day) decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing). [4] Moclobemide (100 mg/kg/day) combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. Moclobemide (100 mg/kg/day) reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

IC50	MAO-A (5-HT), IC50: 6.1 μM
ALogP	1.528
hba_count	2
HBD Count	1
Rotatable Bond	4

关联靶点（人）

MAOB Tclin 胺氧化酶[含黄素]B(Amine oxidase [flavin-containing] B) (1 活性数据)

点击查看靶蛋白信息： MAOB

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

MAOA Tclin 胺氧化酶[含黄素]A(Amine oxidase [flavin-containing] A) (8 活性数据)

点击查看靶蛋白信息： MAOA

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

名称和识别符

分子类型	小分子
Canonical SMILES	ClC1=CC=C(C=C1)C(=O)NCCN2CCOCC2
分子量	268.74
Reaxy-Rn	530974
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=530974&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 70 mg/mL (200.9 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	53
DMSO(mM) Max Solubility	197.22
Water(mg / mL) Max Solubility	<1