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LOX-IN-3 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LOX-IN-3 dihydrochloride图片
CAS NO:2409964-23-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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].

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.
分子量

353.24

性状

Solid

Formula

C13H15Cl2FN2O2S

CAS 号

2409964-23-2

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8309 mL14.1547 mL28.3094 mL
5 mM0.5662 mL2.8309 mL5.6619 mL
10 mM0.2831 mL1.4155 mL2.8309 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。