BML-111

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BML-111 

BML-111 一种脂蛋白 A4 类似物,是一种脂蛋白 A4 (lipoxin A4) 受体激动剂。BML-111 可抑制血管紧张素转化酶 (ACE) 的活性,并增加血管紧张素转化酶 2 (ACE2) 的活性。BML-111 具有抗血管生成,抗肿瘤和抗炎的特性。

BML-111

BML-111 Chemical Structure

CAS No. : 78606-80-1

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生物活性

BML-111, a lipoxin A4 analog, is a lipoxin A4 receptor agonist. BML-111 represses the activity of angiotensin converting enzyme (ACE) and increases the activity of angiotensinconverting enzyme 2 (ACE2). BML-111 has antiangiogenic, antitumor and anti-inflammatory properties[1][2].

IC50 & Target

Lipoxin A4 receptor[1]
Angiotensin converting enzyme (ACE)[2]

体外研究
(In Vitro)

In H22 cells, BML-111 inhibits the production of vascular endothelial growth factor and reduces hypoxia-inducible factor-1α level[1].
BML-111 inhibits leukotriene B4-induced cellular migration with an IC50 of 5 nM[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BML-111 (1 mg/kg; intraperitoneal injection; for 15 days; male Imprinting Control Region mice) treatment suppresses tumor-related angiogenesis and tumor growth in vivo. BML-111 also enhances the in situ apoptosis while inhibiting macrophage infiltration in tumor tissue[1].
BML-111 protects LPS-induced acute lung injury and LPS/D-GalN-induced acute liver injury. BML-111 represses the activity of ACE, but increases the activity of ACE2. BML-111 decreases the expression levels of ACE, AngII, and AngII type 1 receptor (AT1R), meanwhile increases the levels of ACE2, angiotensin-(1-7) (Ang-1-7), and Mas[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Imprinting Control Region mice (5-6-week-old,18-22 g) injected with H22 cells[1]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; injected 5 minutes before and 4 hours after H22 cell inoculation, then every 12 hours for 2 consecutive days, then daily in an additional 3 days and every other day for the last 10 days
Result: Suppressed tumor-related angiogenesis and tumor growth in vivo.

分子量

192.21

Formula

C8H16O5

CAS 号

78606-80-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Ying Chen, et al. Lipoxin A4 and Its Analogue Suppress the Tumor Growth of Transplanted H22 in Mice: The Role of Antiangiogenesis. Mol Cancer Ther. 2010 Aug;9(8):2164-74.

    [2]. Qiong-Feng Chen, et al. BML-111, a Lipoxin Receptor Agonist, Protects Against Acute Injury via Regulating the Renin Angiotensin-Aldosterone System. Prostaglandins Other Lipid Mediat. 2019 Feb;140:9-17.

    [3]. T H Lee, et al. Inhibition of Leukotriene B4-induced Neutrophil Migration by Lipoxin A4: Structure-Function Relationships. Biochem Biophys Res Commun. 1991 Nov 14;180(3):1416-21.

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