1. Immunology/Inflammation
  2. VAP-1
  3. PXS-4681A

PXS-4681A 是一种有效、选择性、不可逆且具有口服活性的氨基脲敏感胺氧化酶 (SSAO; VAP-1) 抑制剂,Ki 为 37 nM。PXS-4681A 对相关的胺氧化酶、离子通道和七跨膜结构域受体显示出高度选择性。PXS-4681A 具有抗炎作用。

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PXS-4681A Chemical Structure

PXS-4681A Chemical Structure

CAS No. : 1478364-87-2

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10 mg ¥4750
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects[1].

IC50 & Target

Ki: 37 nM (SSAO)[1]

体外研究
(In Vitro)

PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively[1].

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

体内研究
(In Vivo)

PXS-4681A (2 mg/kg; PO; single dose) attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung inflammation and localized inflammation[1].
In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies[1].

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

Animal Model: Carrageenan-induced skin inflammation mice[1]
Dosage: 2 mg/kg
Administration: oral administration; single dose
Result: Reduced local inflammation, causing a significant reduction in exudate volume by 25%.
分子量

296.75

Formula

C10H14ClFN2O3S

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 : 250 mg/mL (842.46 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 3.3698 mL 16.8492 mL 33.6984 mL
5 mM 0.6740 mL 3.3698 mL 6.7397 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 3.3698 mL 16.8492 mL 33.6984 mL 84.2460 mL
5 mM 0.6740 mL 3.3698 mL 6.7397 mL 16.8492 mL
10 mM 0.3370 mL 1.6849 mL 3.3698 mL 8.4246 mL
15 mM 0.2247 mL 1.1233 mL 2.2466 mL 5.6164 mL
20 mM 0.1685 mL 0.8425 mL 1.6849 mL 4.2123 mL
25 mM 0.1348 mL 0.6740 mL 1.3479 mL 3.3698 mL
30 mM 0.1123 mL 0.5616 mL 1.1233 mL 2.8082 mL
40 mM 0.0842 mL 0.4212 mL 0.8425 mL 2.1061 mL
50 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6849 mL
60 mM 0.0562 mL 0.2808 mL 0.5616 mL 1.4041 mL
80 mM 0.0421 mL 0.2106 mL 0.4212 mL 1.0531 mL
100 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 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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Inquiry Information

产品名称:
PXS-4681A
目录号:
HY-117833
需求量: