规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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体外研究 (In Vitro) |
LOX-IN-3 二盐酸盐一水合物(化合物 33)对牛 LOX 的 IC50 值小于 10 μM,对人 LOXL2 活性的 IC50 值小于 1 μM [1]。 LOXL1 和 LOXL2 始终受到 LOX-IN-3 二盐酸盐一水合物的抑制 [1]。 LOX-IN-3 二盐酸盐的一水合物相对于 SSAO/VAP-1 和 MAO-B 具有降低的活性 [1]。
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体内研究 (In Vivo) |
LOX-IN-3 二盐酸盐一水合物(化合物 33)(30 mg/kg;口服;一次)抑制大鼠赖氨酰氧化酶活性 [1]。 LOX-IN-3 二盐酸盐一水合物(10 mg/kg;口服;每天一次,持续 14 天)可降低单侧输尿管梗阻 (UUO) 小鼠模型的肾纤维化 [1]。 LOX-IN-3 二盐酸盐一水合物(15 mg/kg;口服;每天一次,持续 21 天)可减少大鼠的肺纤维化 [1]。
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动物实验 |
Animal/Disease Models: Male Wistar rat[1]
Doses: 30 mg/kg Route of Administration: Orally, single dose Experimental Results:Complete elimination of lysyl oxidase activity. Plasma concentrations of the test compound were well below the IC50 after 8 hrs (hrs (hours)), and the recovery half-life was between 2-3 days (ear) and 24 hrs (hrs (hours)) (aorta). Animal/Disease Models: Mouse unilateral ureteral obstruction (UUO) model of acute renal fibrosis [1] Doses: 10 mg/kg Route of Administration: po (oral gavage), one time/day for 14 days Experimental Results: Increased kidney weight and thickness, fiber The area is diminished. Animal/Disease Models: C57Bl/6 mice, bleomycin-induced pulmonary fibrosis model. Doses: 15 mg/kg. Route of Administration: po (oral gavage), one time/day for 21 days. Experimental Results: Dramatically diminished Ashcroft score and lung weight. |
参考文献 |
[1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1.
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分子式 |
C13H14CLFN2O2S
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分子量 |
316.7789
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CAS号 |
2409964-23-2
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相关CAS号 |
LOX-IN-3;2409963-83-1;LOX-IN-3 dihydrochloride monohydrate;2414974-55-1
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SMILES |
Cl[H].S(C([H])([H])/C(=C(\[H])/C([H])([H])N([H])[H])/F)(C1=C([H])C([H])=C([H])C2C([H])=C([H])C([H])=NC1=2)(=O)=O
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
H2O : ≥ 100 mg/mL (~283.09 mM)
DMSO : ~33.33 mg/mL (~94.36 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1568 mL | 15.7838 mL | 31.5676 mL | |
5 mM | 0.6314 mL | 3.1568 mL | 6.3135 mL | |
10 mM | 0.3157 mL | 1.5784 mL | 3.1568 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。