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ATX inhibitor 1 {[allProObj[0].p_purity_real_show]}

货号：A1175078

ATX inhibitor 1 is a potent Autotaxin (ATX) with IC50 values of 1.23nM, 2.18nM and 135nM for FS-3, bis-pNPP, human plasma and LPC cell assays, respectively.

ATX inhibitor 1 化学结构
CAS号：2225892-70-4

ATX inhibitor 1 3D分子结构
CAS号：2225892-70-4

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ATX inhibitor 1 纯度/质量文件产品仅供科研

货号：A1175078 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PDE 亚型比较

产品名称	PDE ↓ ↑	PDE1 ↓ ↑	PDE10A ↓ ↑	PDE2 ↓ ↑	PDE3 ↓ ↑	PDE4 ↓ ↑	PDE5 ↓ ↑	PDE6 ↓ ↑	其他靶点	纯度
Doxofylline	✔									99+%
Deltarasin	+++ PDEδ , Kd: 38 nM									99+%
7-(2,3-Dihydroxypropyl)theophylline	✔									98%
Aminophylline	+ PDE, IC50: 0.12 mM									98+%
Anagrelide HCl	✔									99%+
Irsogladine	✔								AChR,mAChR	98%
PF-8380	+++ Autotaxin, IC50: 2.8 nM									99%+
Dipyridamole	✔									98%
Balipodect			++++ PDE10A, IC50: 0.3 nM							99%+
PF-2545920			++++ PDE10A, IC50: 0.37 nM							97%
Luteolin		+ PDE1, Ki: 15.0 μM		++ PDE2, Ki: 6.4 μM	+ PDE3, Ki: 13.9 μM	+ PDE4, Ki: 11.1 μM	+ PDE5, Ki: 9.5 μM			98%
Milrinone				++ PDE2, IC50: 5.2 μM	++ PDE3, IC50: 2.1 μM				ATPase	98%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				98%
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				98%
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM				98+%
Avanafil							++++ PDE5, IC50: 1 nM			98%
Vardenafil HCl Trihydrate							++++ PDE5, IC50: 0.7 nM			98%
Tadalafil							++++ PDE5, IC50: 1.8 nM			98%
Icariin							++ PDE5, IC50: 0.432 μM			98%
Sildenafil							✔	+++ PDE6, IC50: 33 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ATX inhibitor 1 生物活性

描述

Autotaxin (ATX) is a key enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).Inhibition of ATX decreased estrogen and LPA‑induced cell proliferation. High LPA levels markedly elevated the phosphorylation levels of extracellular signal‑regulated kinase (ERK). ATX downregulation moderately decreased estrogen‑ and LPA‑induced phosphorylation of ERK^[2]. In pulmonary fibrosis, ATX levels rise in the broncheoalveolar fluid (BALF) and stimulate LPA production. LPA engagement of its receptors activate multiple G-protein mediated signal transduction pathways leading to different responses from pulmonary cells including the production of pro-inflammatory signals from stressed epithelial cells, the modulation of endothelial physiology, the activation of TGF signaling and the stimulation of fibroblast accumulation^[3]. Autotaxin (ATX) is a potential target for the treatment of various cancers. ATX inhibitor 1 is a potent ATX inhibitor (IC50: 1.23 nM, FS-3 and 2.18 nM, bis-pNPP)^[1].

ATX inhibitor 1 参考文献

[1]Balupuri A, et al. Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation. Eur J Med Chem. 2018. 148, 397-409.

[2]Guo Zhang,et al. ATX‑LPA axis facilitates estrogen‑induced endometrial cancer cell proliferation via MAPK/ERK signaling pathway. Mol Med Rep. 2018. 17(3), 4245-4252.

[3]Ioanna Ninou,et al. Autotaxin in Pathophysiology and Pulmonary Fibrosis. Front Med (Lausanne). 2018. 5, 180.

ATX inhibitor 1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.95mL

3.99mL

1.99mL

ATX inhibitor 1 技术信息

CAS号	2225892-70-4
分子式	C₂₁H₂₃Cl₂N₂O₆P
分子量	501.297

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 250 mg/mL(498.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

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ATX inhibitor 1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ATX inhibitor 1 质控信息

ATX inhibitor 1 生物活性

ATX inhibitor 1 参考文献

ATX inhibitor 1 实验方案

ATX inhibitor 1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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ATX inhibitor 1 纯度/质量文件产品仅供科研