首页工具

PXS-5153A monohydrochloride

产品编号 T12585L CAS 2125956-82-1

别名: PXS-5153A monohydrochloride (2125956-82-1 free base)

PXS-5153A monohydrochloride 是一种有效的、选择性的、具有口服活性和快速起效的赖氨酰氧化酶 2/3(LOXL2/LOXL3)的双抑制剂，对几乎所有哺乳动物物种 LOXL2的 IC50均< 40 nM，对人类 LOXL3 的 IC50为63 nM。PXS-5153A monohydrochloride 可减少交联并改善纤维化。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

PXS-5153A monohydrochloride Chemical Structure

PXS-5153A monohydrochloride, CAS 2125956-82-1

规格	价格/CNY		货期	数量
50 mg	￥ 13,700		5日内发货
100 mg	￥ 18,700		5日内发货

大包装超大折扣，点击咨询

PXS-5153A monohydrochloride 的其他形式现货产品:

PXS-5153A

其他形式的 PXS-5153A monohydrochloride:

PXS-5153A
现货

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis
体外活性	PXS-5153A shows an IC 50 of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC 50 value of 63 nM. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast-acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes [1].
体内活性	As expected, rhLOXL2 induces collagen oxidation in a dose-dependent manner while PXS-5153A impedes collagen oxidation in a dose-dependent manner. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl 4 treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation compared to the CCl 4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl 4 group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A [1].

别名	PXS-5153A monohydrochloride (2125956-82-1 free base)
分子量	475.41
分子式	C20H25Cl2FN4O2S
CAS No.	2125956-82-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (569.54 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1034 mL	10.5172 mL	21.0345 mL	52.5862 mL
	5 mM	0.4207 mL	2.1034 mL	4.2069 mL	10.5172 mL
	10 mM	0.2103 mL	1.0517 mL	2.1034 mL	5.2586 mL
	20 mM	0.1052 mL	0.5259 mL	1.0517 mL	2.6293 mL
	50 mM	0.0421 mL	0.2103 mL	0.4207 mL	1.0517 mL
	100 mM	0.021 mL	0.1052 mL	0.2103 mL	0.5259 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +