1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-5120A

PXS-5120A 是一种有效的,不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂,具有抗纤维化活性。与 LOXL (pIC50 为 5.8) 相比,PXS-5120A 对 LOXL2 (Ki 为 83 nM; pIC50 为 8.4) 的选择性高 300 倍以上。

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PXS-5120A Chemical Structure

PXS-5120A Chemical Structure

CAS No. : 2125955-70-4

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Customer Review

查看 Monoamine Oxidase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1].

IC50 & Target

pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)[1]

体外研究
(In Vitro)

PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

481.97

Formula

C22H25ClFN3O4S

CAS 号
性状

固体

颜色

White to off-white

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
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (259.35 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0748 mL 10.3741 mL 20.7482 mL
5 mM 0.4150 mL 2.0748 mL 4.1496 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0748 mL 10.3741 mL 20.7482 mL 51.8704 mL
5 mM 0.4150 mL 2.0748 mL 4.1496 mL 10.3741 mL
10 mM 0.2075 mL 1.0374 mL 2.0748 mL 5.1870 mL
15 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4580 mL
20 mM 0.1037 mL 0.5187 mL 1.0374 mL 2.5935 mL
25 mM 0.0830 mL 0.4150 mL 0.8299 mL 2.0748 mL
30 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7290 mL
40 mM 0.0519 mL 0.2594 mL 0.5187 mL 1.2968 mL
50 mM 0.0415 mL 0.2075 mL 0.4150 mL 1.0374 mL
60 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8645 mL
80 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6484 mL
100 mM 0.0207 mL 0.1037 mL 0.2075 mL 0.5187 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PXS-5120A
目录号:
HY-130242
需求量: