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ML351 {[allProObj[0].p_purity_real_show]}

货号:A1002813 同义名: CID 664510

ML351是一种新型的化学类15-LOX-1选择性抑制剂,IC50 为 200 nM,具有较高的选择性 (>250倍) 作用于相关同工酶如 5-LOX、12-LOX、COX-2 等,并且能抑制非肥胖糖尿病小鼠模型中的血糖异常。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
ML351 化学结构 CAS号:847163-28-4
ML351 化学结构
CAS号:847163-28-4
ML351 3D分子结构
CAS号:847163-28-4
ML351 化学结构 CAS号:847163-28-4
ML351 3D分子结构 CAS号:847163-28-4
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ML351 纯度/质量文件 产品仅供科研

货号:A1002813 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 lipoxygenase 其他靶点 纯度
Zileuton 97%
Nordihydroguaiaretic acid 99%+
MK-886 99%+
Esculetin 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ML351 生物活性

描述 ML351 is a novel chemotype and the first reported selective inhibitor of 15-LOX-1 with IC50 value of 200 nM. It is a tight binding, mixed inhibitor which could protect against oxidative glutamate toxicity in mouse neuronal cells (HT-22) and significantly reduced infarct size in an in vivo mouse model for ischemic stroke.

ML351 细胞实验

Cell Line
Concentration Treated Time Description References
mouse islets 10 μmol/L 24 hours ML351 reduced 12-HETE release and improved glucose-stimulated insulin secretion. Diabetes. 2017 Nov;66(11):2875-2887
Keratinocytes in human skin equivalents 10 µM 24 or 48 hours ML351 significantly elevated the secretion of CCL2, CCL5, and CXCL10, indicating its enhancement of keratinocyte inflammatory responses. Cell Death Dis. 2025 Jan 22;16(1):39
NHEK/SVTERT3-5 cells 10 µM 24 hours ML351 significantly reduced many metabolites of arachidonic and linoleic acid, indicating its inhibition of lipoxygenase activity. Cell Death Dis. 2025 Jan 22;16(1):39
Primary spinal microglia 100 ng/ml 8 and 24 hours To assess the effect of KLA treatment on 15-LOX-1 protein expression. KLA treatment significantly upregulated 15-LOX-1 protein expression in microglia. Pain. 2018 Dec;159(12):2620-2629
HEK-293T cells 0.1 nM-10 μM 30 minutes To evaluate the inhibitory effects of ML351 and ML127 on 15-LOX-1 and 12-LOX-p activity. ML351 significantly inhibited the activity of 15-LOX-1 and 12-LOX-p at low nanomolar concentrations, while ML127 preferentially reduced 15-LOX-1 activity. Pain. 2018 Dec;159(12):2620-2629
human lung macrophages 10 μM 24 hours To evaluate the inhibitory effect of ML351 on chemokine release induced by LPS and Th2 cytokines. Results showed that ML351 significantly inhibited LPS-induced release of CCL2 and CCL3, as well as IL-4-induced release of CCL13 and CCL22. Br J Pharmacol. 2015 Sep;172(17):4319-30

ML351 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Streptozotocin (STZ)-induced type 1 diabetes model Intraperitoneal injection 10, 24, 48 mg/kg Once daily, starting 5 days before STZ and ending 5 days after the last STZ dose ML351 (10 and 24 mg/kg) prevented diabetes development, reduced β-cell oxidative stress, and preserved β-cell mass. The 48 mg/kg dose was ineffective. Diabetes. 2017 Nov;66(11):2875-2887
Mice Subarachnoid hemorrhage model Intraperitoneal injection 50 mg/kg Administered 5 minutes after SAH induction, assessed 1 and 3 days later To evaluate the impact of ML351 on brain injury after SAH. Results showed that ML351 reduced neuronal cell death and improved neurological outcomes. Stroke. 2019 Feb;50(2):520-523
C57BL6J mice Transient middle cerebral artery occlusion (MCAO) model Intraperitoneal injection 50 mg/kg Single dose ML351 reduced hemorrhagic transformation (HT) in wild-type mice and similarly reduced HT following tPA treatment Stroke. 2017 Feb;48(2):445-451
Male Holtzman Sprague-Dawley rats TLR4-dependent NSAID-unresponsive hyperalgesia model Intrathecal injection 0.1–10 μg/10 μl Single injection, 30 minutes pretreatment To evaluate the inhibitory effects of ML351 and ML127 on TLR4-mediated hyperalgesia. ML351 significantly attenuated hyperalgesia at all tested doses, while ML127 showed dose-dependent inhibition at high doses. Pain. 2018 Dec;159(12):2620-2629
Mice LepRdb/db mice (type 2 diabetes model) Intraperitoneal injection 100mg/kg 7 consecutive days To evaluate the effect of ML351 on vascular function and diastolic function in diabetic mice, results showed that ML351 improved endothelium-dependent vasodilation and left ventricular diastolic function Life Sci. 2021 Nov 1;284:119925
Male Swiss Albino mice Ischemia/recanalization (I/R) model Intraperitoneal injection 50 mg/kg Single dose at recanalization To investigate the effects of ML351 on ischemia/recanalization-induced neuroinflammation. Results showed that ML351 significantly reduced infarct volume, neurological deficit score, and lipid peroxidation, and suppressed inflammasome (NLRP1 and NLRP3) activation. Front Cell Neurosci. 2023 Sep 26;17:1277268
Mice Alox12 knockout mice Intraperitoneal injection 10 mg/kg body weight 5 days prior to STZ treatment, during treatment, and 5 days post-STZ treatment, daily administration To evaluate the protective effect of ML351 on STZ-induced glucose intolerance, results showed that ML351 treatment significantly improved glucose tolerance in Alox12 knockout mice J Biol Chem. 2019 Apr 19;294(16):6612-6620

ML351 参考文献

[1]Ganesha Rai, Netra Joshi, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1.

ML351 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.06mL

4.01mL

2.01mL

40.12mL

8.02mL

4.01mL

ML351 技术信息

CAS号847163-28-4
分子式C15H11N3O
分子量 249.27
SMILES Code N#CC1=C(NC)OC(C2=C3C=CC=CC3=CC=C2)=N1
MDL No. MFCD04183120
别名 CID 664510
运输蓝冰
InChI Key DYXYXTDIFMDJIR-UHFFFAOYSA-N
Pubchem ID 664510
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 50 mg/mL(200.59 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
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