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。
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| 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+ |


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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。 | |||||||||||||||||||
| 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. |
| 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 |
| 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 |
| 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 |
|
| 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 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
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