LOX-IN-3 dihydrochloride 是一种具有口服活性的赖氨酰氧化酶 (lysyl oxidase (LOX)) 抑制剂,可用于纤维化,癌症和血管生成研究。
生物活性 | LOX-IN-3 dihydrochloride is an orally activelysyl oxidase (LOX)inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis,cancerand angiogenesis research[1]. |
IC50& Target | IC50:<1 μm (human loxl2),<10 (bovine lox)[1] |
体外研究 (In Vitro) | LOX-IN-3 dihydrochloride monohydrate (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50values of<10 μm and<1 μm, respectively[1]. LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2[1]. LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities[1].
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体内研究 (In Vivo) | LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1]. LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1]. LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1].
Animal Model: | Male Wistar rats[1] | Dosage: | 30 mg/kg | Administration: | Oral administration, single dose | Result: | Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta). |
Animal Model: | Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice[1] | Dosage: | 10 mg/kg | Administration: | Oral gavage, daily for 14 days | Result: | Increased kidney weight and thickness and reduced the area of fibrosis. |
Animal Model: | C57Bl/6 mice, Bleomycin-induced lung fibrosis model | Dosage: | 15 mg/kg | Administration: | Oral gavage, daily for 21 days | Result: | Significantly reduced the Ashcroft score and the lung weight. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : ≥ 100 mg/mL(283.09 mM) DMSO : 33.33 mg/mL(94.36 mM;ultrasonic and warming and heat to 80℃) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.8309 mL | 14.1547 mL | 28.3094 mL | 5 mM | 0.5662 mL | 2.8309 mL | 5.6619 mL | 10 mM | 0.2831 mL | 1.4155 mL | 2.8309 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.08 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.08 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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