1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PAT-505

PAT-505 

目录号: HY-107781 纯度: 98.01%
产品使用指南

PAT-505 是一种有效,选择性的,非竞争性的可口服的 autotaxin 抑制剂,在 Hep3B 中,抑制 autotaxin 的活性,IC50 值为 2 nM,在人血液和小鼠血浆中,IC50 值分别为 9.7 nM 和 62 nM。

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PAT-505 Chemical Structure

PAT-505 Chemical Structure

CAS No. : 1782070-22-7

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
5 mg ¥5500
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10 mg ¥8500
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50 mg ¥28500
In-stock
100 mg ¥39500
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.

IC50 & Target[1]

Autotaxin

2 nM (IC50, In Hep3B cells)

Autotaxin

9.7 nM (IC50, In human blood )

Autotaxin

62 nM (IC50, In mouse plasma)

体外研究
(In Vitro)

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. PAT-505 is selective for ATX versus other ENPP proteins, and shows marginal inhibition of radiolabeled agonist or antagonist binding to the adenosine A3 receptor, MT1 melatonin receptor, prostaglandin E2 EP4 receptor, 5-HT5a serotonin receptor, and GABA-gated Cl- channel with 50%-70% inhibition at 10 µM[1].

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

体内研究
(In Vivo)

PAT-505 suppresses ATX lysoPLD activity with an average IC50 value of 62 nM and an average IC90 value of 630 nM in mouse plasma, and the IC90 in rat plasma is ∼770 nM. PAT-505 (30 mg/kg, p.o.) significantly reduces fibrotic score, the percentage of PSR-positive area, and α-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH)[1].

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

分子量

473.92

Formula

C23H18ClF2N3O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 48.33 mg/mL (101.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1101 mL 10.5503 mL 21.1006 mL
5 mM 0.4220 mL 2.1101 mL 4.2201 mL
10 mM 0.2110 mL 1.0550 mL 2.1101 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°C, 6 months; -20°C, 1 month。-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。

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: ≥ 4.83 mg/mL (10.19 mM); Clear solution

    此方案可获得 ≥ 4.83 mg/mL (10.19 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 48.3 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% corn oil

    Solubility: ≥ 4.83 mg/mL (10.19 mM); Clear solution

    此方案可获得 ≥ 4.83 mg/mL (10.19 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 48.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[1]

Mice[1]
NASH is induced in male C57BL/6 mice. Briefly, 5-week-old mice are acclimated for 1 week on normal chow before switching to a choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD) containing 60% kcal% fat and 0.1% methionine. After 4 weeks of CDAHFD feeding, approximately 200 μL of blood is collected from each animal via a submandibular bleed and the serum analyzed for liver enzyme levels. Any animal with a total serum bilirubin level >1 mg/dL is removed from the study prior to compound dosing. Animals are fed CDAHFD for 5 weeks before randomization into treatment groups (n = 7-10 per group). Vehicle or PAT-505 (3-30 mg/kg) is administered by oral gavage in 0.5% methylcellulose (MC) once daily from weeks 5 to 12[1].

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

参考文献

纯度: 99.47%

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The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
PAT-505
目录号:
HY-107781
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