LOX-IN-3 dihydrochloride

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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。

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 mg

5 mg

10 mg

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。
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。